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  • 1. Ahlberg, P.
    et al.
    Karlsson, A.
    Goeppert, A.
    Lill, S. O. N.
    Dinér, Peter
    Sommer, J.
    Solvated CH5+ in liquid superacid2001Inngår i: Chemistry - A European Journal, ISSN 0947-6539, E-ISSN 1521-3765, Vol. 7, nr 12, s. 2501-2510Artikkel i tidsskrift (Fagfellevurdert)
  • 2. Alao, John Patrick
    et al.
    Michlíková, Sona
    Dinér, Peter
    KTH, Skolan för kemivetenskap (CHE), Kemi, Organisk kemi. Gothenburg University.
    Grøtli, Morten
    Sunnerhagen, Per
    Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP862014Inngår i: BMC Cancer, ISSN 1471-2407, E-ISSN 1471-2407, Vol. 14, nr 853Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    Background

    The RET tyrosine kinase receptor has emerged as a target in thyroid and endocrine resistant breast cancer. We previously reported the synthesis of kinase inhibitors with potent activity against RET. Herein, we have further investigated the effect of the lead compound SPP86 on RET mediated signaling and proliferation. Based on these observations, we hypothesized that SPP86 may be useful for studying the cellular activity of RET.

    Methods

    We compared the effects of SPP86 on RET-induced signaling and proliferation in thyroid cancer cell lines expressing RET-PTC1 (TPC1), or the activating mutations BRAFV600E (8505C) and RASG13R (C643). The effect of SPP86 on RET- induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK pathway signaling and cell proliferation in MCF7 breast cancer cells was also investigated.

    Results

    SPP86 inhibited MAPK signaling and proliferation in RET/PTC1 expressing TPC1 but not 8505C or C643 cells. In TPC1 cells, the inhibition of RET phosphorylation required co-exposure to SPP86 and the focal adhesion kinase (FAK) inhibitor PF573228. In MCF7 cells, SPP86 inhibited RET- induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling and estrogen receptorα (ERα) phosphorylation, and inhibited proliferation to a similar degree as tamoxifen. Interestingly, SPP86 and PF573228 inhibited RET/PTC1 and GDNF- RET induced activation of Akt and MAPK signaling to a similar degree.

    Conclusion

    SPP86 selectively inhibits RET downstream signaling in RET/PTC1 but not BRAFV600E or RASG13R expressing cells, indicating that downstream kinases were not affected. SPP86 also inhibited RET signaling in MCF7 breast cancer cells. Additionally, RET- FAK crosstalk may play a key role in facilitating PTC1/RET and GDNF- RET induced activation of Akt and MAPK signaling in TPC1 and MCF7 cells.

  • 3. Amorati, Riccardo
    et al.
    Valgimigli, Luca
    Dinér, Peter
    Bakhtiari, Khadijeh
    Saeedi, Mina
    Engman, Lars
    Multi-faceted reactivity of alkyltellurophenols towards peroxyl radicals: Catalytic antioxidant versus thiol-depletion effect2013Inngår i: Chemistry - A European Journal, ISSN 0947-6539, E-ISSN 1521-3765, Vol. 19, nr 23, s. 7510-7522Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    Hydroxyaryl alkyl tellurides are effective antioxidants both in organic solution and aqueous biphasic systems. They react by an unconventional mechanism with ROO. radicals with rate constants as high as 107 M−1 s−1 at 303 K, outperforming common phenols. The reactions proceed by oxygen atom transfer to tellurium followed by hydrogen atom transfer to the resulting RO. radical from the phenolic OH. The reaction rates do not reflect the electronic properties of the ring substituents and, because the reactions occur in a solvent cage, quenching is more efficient when the OH and TeR groups have an ortho arrangement. In the presence of thiols, hydroxyaryl alkyl tellurides act as catalytic antioxidants towards both hydroperoxides (mimicking the glutathione peroxidases) and peroxyl radicals. The high efficiency of the quenching of the peroxyl radicals and hydroperoxides could be advantageous under normal cellular conditions, but pro-oxidative (thiol depletion) when thiol concentrations are low.

  • 4. Bertelsen, Søren
    et al.
    Dinér, Peter
    Johansen, Rasmus Lyng
    Jørgensen, Karl Anker
    Asymmetric organocatalytic beta-hydroxylation of alpha, beta-unsaturated aldehydes2007Inngår i: Journal of the American Chemical Society, ISSN 0002-7863, E-ISSN 1520-5126, Vol. 129 1536-1537, nr 6, s. 1536-1537Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    The first catalytic enantioselective β-hydroxylation of α,β-unsaturated aldehydes is presented. Using commercially available (E)-benzaldehyde oxime in the presence of 2-[bis(3,5-bis-trifluoromethyl-phenyl)trimethyl-silanyloxymethyl]pyrrolidine as organocatalyst, the corresponding chiral carbonyl β-oxime ethers are obtained in high yields and with excellent enantioselectivities. These optically active carbonyl and hydroxy β-oxime ethers are highly interesting biological compounds in, e.g., sex pheromone analogues, highly potent antiinflammatory agents, and penicillin and cephalosporin analogues. The chiral carbonyl β-oxime ethers can be reduced to the corresponding 1,3-diols in high yields. Furthermore, the organocatalytic enantioselective β-hydroxylation of α,β-unsaturated aldehydes could be performed on gram scale without loss of enantioselectivity.

  • 5. Bertelsen, Søren
    et al.
    Marigo, Mauro
    Brandes, Sebastian
    Dinér, Peter
    Jørgensen, Karl Anker
    Dienamine catalysis: organocatalytic asymmetric gamma-amination of alpha,beta-unsaturated aldehydes2006Inngår i: Journal of the American Chemical Society, ISSN 0002-7863, E-ISSN 1520-5126, Vol. 128, nr 39, s. 12973-12980Artikkel i tidsskrift (Fagfellevurdert)
  • 6.
    Blomkvist, Björn
    et al.
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi.
    Dinér, Peter
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi.
    HBF4 center dot DEE-catalyzed formation of sulfinyl imines: Synthesis and mechanistic studies2018Inngår i: Tetrahedron Letters, ISSN 0040-4039, E-ISSN 1359-8562, Vol. 59, nr 13, s. 1249-1253Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    A mild acid-catalysed method is reported for the formation of sulfinyl imines from tert-butanesulfinamide and aromatic or aliphatic aldehydes using tetrafluoroboric acid diethyletherate (10 mol%) in dichloromethane. Reactions were performed at room temperature and gave the corresponding sulfinyl imines in excellent yield after 2 h. A DFT study was performed and a mechanism for the reaction is postulated. 

  • 7.
    Blomkvist, Björn
    et al.
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi.
    Dinér, Peter
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi.
    HBF4·DEE-catalyzed formation of sulfinyl imines: Synthesis and mechanistic studies2018Inngår i: Tetrahedron Letters, ISSN 0040-4039, E-ISSN 1359-8562, Vol. 59, s. 1249-1253Artikkel i tidsskrift (Fagfellevurdert)
  • 8.
    Blomkvist, Björn
    et al.
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Dinér, Peter
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Mild and Rapid Aniline/HBF4 center dot DEE-Catalysed Formation of Sulfinyl Imines2019Inngår i: ChemistrySelect, ISSN 2365-6549, Vol. 4, nr 25, s. 7431-7436Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    The combination of anline and tetrafluoroboric acid diethyl etherate (2.5 mol% and 5 mol%, respectively) significantly accelerates the formation of sulfinyl imines in dichloromethane and isopropylacetate at room temperature compared to previous procedures. A DFT and NMR spectroscopic study shows that the anilinium tetrafluoroborate complex is solvated by sulfinamide molecules in the initial state and that the rate-limiting step of the reaction is the addition of the sulfinamide molecule to the protonated aniline-based imine. In addition, the catalytic system was also utilised in a one-pot, two step reaction, where the in situ formed sulfinyl imine was arylated in a rhodium catalysed reaction with high diastereoselectivity.

  • 9.
    Blomkvist, Björn
    et al.
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Dinér, Peter
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Mild and Rapid Aniline/HBF4•DEE‐Catalysed Formation of Sulfinyl Imines2019Inngår i: ChemistrySelectArtikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    The combination of anline and tetrafluoroboric acid diethyl etherate (2.5 mol% and 5 mol%, respectively) significantly accelerates the formation of sulfinyl imines in dichloromethane and isopropylacetate at room temperature compared to previous procedures. A DFT and NMR spectroscopic study shows that the anilinium tetrafluoroborate complex is solvated by sulfinamide molecules in the initial state and that the rate‐limiting step of the reaction is the addition of the sulfinamide molecule to the protonated aniline‐based imine. In addition, the catalytic system was also utilised in a one‐pot, two step reaction, where the in situ formed sulfinyl imine was arylated in a rhodium catalysed reaction with high diastereoselectivity.

  • 10.
    Blomkvist, Björn
    et al.
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Dinér, Peter
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Josephson, Philip
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Qasim, Wafa
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Nykvist, Viktor
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Student-Driven Development of Greener Chemistry in Undergraduate Teaching: Synthesis of Lidocaine Revisited2019Inngår i: Journal of Chemical Education, s. 1389-1394Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    Green chemistry and sustainable development have become increasingly important topics for the education of future chemists, but the implementation of green chemistry into the chemistry curriculum requires significant efforts from teachers, especially in laboratory education. A student-driven development of a greener synthesis of Lidocaine was performed by three first-cycle, third-year students as a part of their B. Sc. degree project with the goal to implement the procedure in an under-graduate organic chemistry course. The students were merely provided with the framework for the project and were given the opportunity to independently develop the project based on an analysis of the 12 principles of green chemistry. The "greenification" of the Lidocaine synthesis by the three students led to several green improvements of the standard procedure, for example, (1) decreased reaction temperature, (2) solvent replacement, (3) fewer equivalents of the starting material (diethylamine) by the use of an inorganic bulk base, (4) use of catalytic amounts of potassium iodide to promote the Finkelstein reaction, and (5) a two-step one-pot procedure. Furthermore, one of the developed procedures was successfully implemented in a full-scale organic chemistry laboratory course.

  • 11. Diaz-Alvarez, Alba E.
    et al.
    Mesas-Sanchez, Laura
    Dinér, Peter
    KTH, Skolan för kemivetenskap (CHE), Kemi, Organisk kemi. Uppsala University, Sweden.
    Access to Optically Pure beta-Hydroxy Esters via Non-Enzymatic Kinetic Resolution by a Planar-Chiral DMAP Catalyst2014Inngår i: Molecules, ISSN 1420-3049, E-ISSN 1420-3049, Vol. 19, nr 9, s. 14273-14291Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    The development of new approaches to obtain optically pure beta-hydroxy esters is an important area in synthetic organic chemistry since they are precursors of other high value compounds. Herein, the kinetic resolution of racemic beta-hydroxy esters using a planar-chiral DMAP derivative catalyst is presented. Following this procedure, a range of aromatic beta-hydroxy esters was obtained in excellent selectivities (up to s = 107) and high enantiomeric excess (up to 99% ee). Furthermore, the utility of the present method was demonstrated in the synthesis of (S)-3-hydroxy-N-methyl-3-phenylpropanamide, a key intermediate for bioactive molecules such as fluoxetine, tomoxetine or nisoxetine, in its enantiomerically pure form.

  • 12. Dierckx, Anke
    et al.
    Dinér, Peter
    Department of Chemistry, Medicinal Chemistry, University of Gothenburg.
    El-Sagheer, A. H.
    Kumar, Joshi Dhruval
    Brown, T.
    Grøtli, Morten
    Wilhelmsson, Marcus
    Wilhelmsson, L Marcus
    Characterization of photophysical and base-mimicking properties of a novel fluorescent adenine analogue in DNA2011Inngår i: Nucleic Acids Research, ISSN 0305-1048, E-ISSN 1362-4962, Vol. 34, nr 10, s. 4513-4524Artikkel i tidsskrift (Fagfellevurdert)
  • 13.
    Dinér, Peter
    University of Gothenburg.
    Alkane activation by superacids and enantioselective reactions with chiral lithium amides: computational and experimental mechanistic studies2005Doktoravhandling, med artikler (Annet vitenskapelig)
  • 14.
    Dinér, Peter
    Uppsala University.
    Catalytic asymmetric chiral lithium amide-promoted epoxide rearrangement: a NMR spectroscopic and kinetic investigation2010Inngår i: Tetrahedron: asymmetry, ISSN 0957-4166, E-ISSN 1362-511X, Vol. 21, nr 21-22, s. 2733-2739Artikkel i tidsskrift (Fagfellevurdert)
  • 15.
    Dinér, Peter
    Uppsala University.
    Superacid-Promoted Ionization of Alkanes Without Carbonium Ion Formation: A Density Functional Theory Study2012Inngår i: Journal of Physical Chemistry A, ISSN 1089-5639, E-ISSN 1520-5215, Vol. 116, nr 40, s. 9979-9984Artikkel i tidsskrift (Fagfellevurdert)
  • 16.
    Dinér, Peter
    KTH, Skolan för kemivetenskap (CHE), Kemi, Organisk kemi.
    Yttrium from Ytterby2016Inngår i: Nature Chemistry, ISSN 1755-4330, E-ISSN 1755-4349, Vol. 8, nr 2, s. 192-192Artikkel i tidsskrift (Fagfellevurdert)
  • 17.
    Dinér, Peter
    et al.
    University of Gothenburg.
    Alao, John Patrick
    Söderlund, Johan
    Sunnerhagen, Per
    Grøtli, Morten
    Preparation of 3-Substituted-1-Isopropyl-1H-pyrazolo 3,4-d pyrimidin-4-amines as RET Kinase Inhibitors2012Inngår i: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 55 4872-4876, nr 10, s. 4872-4876Artikkel i tidsskrift (Fagfellevurdert)
  • 18.
    Dinér, Peter
    et al.
    Department of Chemistry, University of Gothenburg.
    Amedjkouh, Mohamed
    Aminophosphonates as organocatalysts in the direct asymmetric aldol reaction towards syn selectivity in the presence of Lewis bases2006Inngår i: Organic and biomolecular chemistry, ISSN 1477-0520, E-ISSN 1477-0539, Vol. 4, nr 11, s. 2091-2096Artikkel i tidsskrift (Fagfellevurdert)
  • 19.
    Dinér, Peter
    et al.
    University of Gothenburg.
    Andersson, T.
    Kjellén, J.
    Elbing, K.
    Hohmann, S.
    Grotli, M.
    Short cut to 1,2,3-triazole-based p38 MAP kinase inhibitors via [3+2]-cycloaddition chemistry2009Inngår i: New Journal of Chemistry, ISSN 1144-0546, E-ISSN 1369-9261, Vol. 331010-1016, nr 5, s. 1010-1016Artikkel i tidsskrift (Fagfellevurdert)
  • 20.
    Dinér, Peter
    et al.
    Danish National Research Foundation, Aarhus University.
    Kjaersgaard, Anne
    Lie, Mette Alstrup
    Jørgensen, Karl Anker
    On the origin of the stereoselectivity in organocatalysed reactions with trimethylsilyl-protected Diarylprolinol2008Inngår i: Chemistry - A European Journal, ISSN 0947-6539, E-ISSN 1521-3765, Vol. 14, nr 1, s. 122-127Artikkel i tidsskrift (Fagfellevurdert)
  • 21.
    Dinér, Peter
    et al.
    Danish National Research Foundation, Aarhus University.
    Nielsen, Martin
    Bertelsen, Søren
    Niess, Barbara
    Jørgensen, Karl Anker
    Enantioselective hydroxylation of nitroalkenes: an organocatalytic approach2007Inngår i: Chemical Communications, ISSN 1359-7345, E-ISSN 1364-548X, nr 35, s. 3646-3648Artikkel i tidsskrift (Fagfellevurdert)
  • 22.
    Dinér, Peter
    et al.
    Danish National Research Foundation, Aarhus University.
    Nielsen, Martin
    Marigo, Mauro
    Jørgensen, Karl Anker
    Enantioselective organocatalytic conjugate addition of N heterocycles to alpha,beta-unsaturated aldehydes2007Inngår i: Angewandte Chemie International Edition, ISSN 1433-7851, E-ISSN 1521-3773, Vol. 46, nr 12, s. 1983-1987Artikkel i tidsskrift (Fagfellevurdert)
  • 23.
    Dinér, Peter
    et al.
    University of Gothenburg.
    Pettersen, Daniel
    Nilsson Lill, Sten O.
    Ahlberg, Per
    Investigation of site selectivity of the stereoselective deprotonation of cyclohexene oxide using kinetic resolution of isotopic enantiomers in natural abundance2005Inngår i: Tetrahedron: asymmetry, ISSN 0957-4166, E-ISSN 1362-511X, Vol. 162665-2671, nr 15, s. 2665-2671Artikkel i tidsskrift (Fagfellevurdert)
  • 24.
    Dinér, Peter
    et al.
    KTH, Skolan för kemivetenskap (CHE), Kemi.
    Sadhukhan, Arghya
    KTH, Skolan för kemivetenskap (CHE), Kemi.
    Blomkvist, Björn
    KTH, Skolan för kemivetenskap (CHE), Kemi.
    Chiral Sulfinamides as Highly Enantioselective Organocatalysts2014Inngår i: ChemCatChem, ISSN 1867-3880, E-ISSN 1867-3899, Vol. 6, nr 11, s. 3063-3066Artikkel i tidsskrift (Fagfellevurdert)
  • 25.
    Dinér, Peter
    et al.
    University of Gothenburg.
    Veide Vilg, Jenny
    Kjellén, Jimmy
    Andersson, Terese
    Hohmann, Stefan
    Tamás, Markus J.
    Grøtli, Morten
    Highly selective, cell-permeable and fast-acting wild-type Hog1 inhibitors as tools for studying cellular function of kinases2009Inngår i: Functional Genomics Symposium: Chemical Biology – Molecules to Probe Life, Gothenburg, Sweden, University of Gothenburg , 2009Konferansepaper (Fagfellevurdert)
  • 26.
    Dinér, Peter
    et al.
    University of Gothenburg.
    Veide Vilg, Jenny
    Kjellén, Jimmy
    Migdal, Iwona
    Andersson, Terese
    Gebbia, Marinella
    Giaever, Guri
    Nislow, Corey
    Hohmann, Stefan
    Wysocki, Robert
    Tamás, Markus J.
    Grøtli, Morten
    Design, synthesis, and characterization of a highly effective Hog1 inhibitor: a powerful tool for analyzing MAP kinase signaling in yeast2011Inngår i: PLoS ONE, ISSN 1932-6203, E-ISSN 1932-6203, Vol. 6, nr 5Artikkel i tidsskrift (Fagfellevurdert)
  • 27. Dinér, Peter
    et al.
    Veide Vilg, Jenny
    Kjellén, Jimmy
    Migdal, Iwona
    Andersson, Therese
    Hohmann, Stefan
    Wysocki, Robert
    Tamás, Markus J.
    Grøtli, Morten
    Design, synthesis and characterization of a highly effective Hog1 inhibitor: a powerful tool for analyzing MAP kinase signalling in yeast2010Inngår i: Yeast Genetics and Molecular Biology Meeting, Vancouver, Canada, 2010Konferansepaper (Fagfellevurdert)
  • 28. Dinér, Peter
    et al.
    Vilg, J V
    Kjellen, J
    Iwona, M
    Andersson, T
    Hohmann, S
    Wysocki, R
    Tamas, M J
    Grotli, M
    Design, synthesis and characterization of a highly effective Hog1 inhibitor: a powerful tool for analyzing MAP kinase signaling in yeast2010Inngår i: Special Issue: Abstracts of the 35th FEBS Congress, Gothenburg, Sweden, 26 June - 1 July 2010, Wiley-Blackwell, 2010, Vol. 277Konferansepaper (Annet vitenskapelig)
  • 29. Dyrager, Christine
    et al.
    Börjesson, Karl
    Dinér, Peter
    University of Gothenburg.
    Elf, A.
    Albinsson, Bo
    Wilhelmsson, Marcus
    Grøtli, Morten
    Synthesis and Photophysical Characterisation of Fluorescent 8-(1H-1,2,3-Triazol-4-yl)adenosine Derivatives2009Inngår i: European Journal of Organic Chemistry, ISSN 1434-193X, E-ISSN 1099-0690, nr 10, s. 1515-1521Artikkel i tidsskrift (Fagfellevurdert)
  • 30. Dyrager, Christine
    et al.
    Nilsson Möllers, Linda
    Kjäll, Linda Karlsson
    Alao, John Patrick
    Dinér, Peter
    University of Gothenburg.
    Wallner, Fredrik
    Sunnerhagen, Per
    Grøtli, Morten
    Möllers, Linda N
    Design, synthesis, and biological evaluation of chromone-based p38 MAP kinase inhibitors2011Inngår i: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 54Artikkel i tidsskrift (Fagfellevurdert)
  • 31. Díaz-Álvarez, Alba E.
    et al.
    Mesas Sanchez, Laura
    Dinér, Peter
    Uppsala University.
    Non-Enzymatic Dynamic Kinetic Resolution of Secondary Aryl Alcohols: Planar Chiral Ferrocene and Ruthenium Catalysts in Cooperation2013Inngår i: Angewandte Chemie International Edition, ISSN 1433-7851, E-ISSN 1521-3773, Vol. 52502-504, nr 2, s. 502-504Artikkel i tidsskrift (Fagfellevurdert)
  • 32. Díaz-Álvarez, Alba E.
    et al.
    Mesas-Sánchez, Laura
    Dinér, Peter
    Uppsala University.
    Nichtenzymatische dynamische kinetische Racematspaltung sekundärer Arylalkohole: planar-chirale Ferrocen- und Rutheniumkatalysatoren im Zusammenspiel2013Inngår i: Angewandte Chemie International Edition, ISSN 1433-7851, E-ISSN 1521-3773, Vol. 125, nr 2, s. 522-524Artikkel i tidsskrift (Fagfellevurdert)
  • 33. Goeppert, Alain
    et al.
    Dinér, Peter
    Göteborg University.
    Ahlberg, Per
    Sommer, Jean
    Methane activation and oxidation in sulfuric acid2002Inngår i: Chemistry - A European Journal, ISSN 0947-6539, E-ISSN 1521-3765, Vol. 8, nr 14, s. 3277-3283Artikkel i tidsskrift (Fagfellevurdert)
  • 34. Hamngren Blomqvist, Charlotte
    et al.
    Dinér, Peter
    KTH, Skolan för kemivetenskap (CHE), Kemi, Organisk kemi.
    Grøtli, Morten
    Goksör, Mattias
    Adiels, Caroline B.
    A Single-Cell Study of a Highly Effective Hog1 Inhibitor for in Situ Yeast Cell Manipulation2014Inngår i: Micromachines, ISSN 2072-666X, E-ISSN 2072-666X, Vol. 5, nr 1, s. 81-96Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    We present a single cell study of a highly effective Hog1 inhibitor. For this application, we used sequential treatment of a Saccharomyces cerevisiae cell array, with the Hog1 inhibitor and osmotic stress. For this purpose, a four-inlet microfluidic chamber with controlled introduction of two different cell strains within the same experimental setting and a subsequent rapid switching between treatments was designed. Multiple cell strains within the same experiment is a unique feature which is necessary for determining the expected absent cellular response. The nuclear translocation of the cytosolic MAPK, Hog1, was monitored by fluorescence imaging of Hog1-GFP on a single-cell level. An optical tweezers setup was used for controlled cell capture and array formation. Nuclear Hog1-GFP localization was impaired for treated cells, providing evidence of a congenial microfluidic setup, where the control cells within the experiments validated its appropriateness. The chamber enables multiple treatments with incubation times in the order of seconds and the possibility to remove either of the treatments during measurement. This flexibility and the possibility to use internal control cells ensures it a valuable scientific tool for unraveling the HOG pathway, similar signal transduction pathways and other biological mechanisms where temporal resolution and real time imaging is a prerequisite.

  • 35. Hamngren Blomqvist, Charlotte
    et al.
    Dinér, Peter
    Department of Chemistry – BMC, Uppsala university.
    Grøtli, Morten
    Goksör, Mattias
    Adiels, Caroline B.
    Hamngren, C.
    Design and evaluation of a microfluidic system for inhibition studies of yeast cell signaling2012Inngår i: Proceedings of SPIE: Optical Trapping and Optical Micromanipulation IX / [ed] Kishan Dholakia and Gabriel C. Spalding, SPIE - International Society for Optical Engineering, 2012, Vol. 8458, s. 84582K-Konferansepaper (Fagfellevurdert)
    Abstract [en]

    In cell signaling, different perturbations lead to different responses and using traditional biological techniques that result in averaged data may obscure important cell-to-cell variations. The aim of this study was to develop and evaluate a four-inlet microfluidic system that enables single-cell analysis by investigating the effect on Hog1 localization post a selective Hog1 inhibitor treatment during osmotic stress. Optical tweezers was used to position yeast cells in an array of desired size and density inside the microfluidic system. By changing the flow rates through the inlet channels, controlled and rapid introduction of two different perturbations over the cell array was enabled. The placement of the cells was determined by diffusion rates flow simulations. The system was evaluated by monitoring the subcellular localization of a fluorescently tagged kinase of the yeast “High Osmolarity Glycerol” (HOG) pathway, Hog1-GFP. By sequential treatment of the yeast cells with a selective Hog1 kinase inhibitor and sorbitol, the subcellular localization of Hog1-GFP was analysed on a single-cell level. The results showed impaired Hog1-GFP nuclear localization, providing evidence of a congenial design. The setup made it possible to remove and add an agent within 2 seconds, which is valuable for investigating the dynamic signal transduction pathways and cannot be done using traditional methods. We are confident that the features of the four-inlet microfluidic system will be a valuable tool and hence contribute significantly to unravel the mechanisms of the HOG pathway and similar dynamic signal transduction pathways.

  • 36.
    Hertzberg, Robin
    et al.
    KTH, Skolan för kemivetenskap (CHE), Kemi.
    Dinér, Peter
    KTH, Skolan för kemivetenskap (CHE), Kemi. Division of Organic Chemistry .
    Moberg, Christina
    KTH, Skolan för kemivetenskap (CHE), Kemi.
    Palladium-Catalyzed C(sp3)–C(sp2) Cross-Couplings of O-(α-Bromoacyl) Cyanohydrins with Boronic Acids: An Entry to Enantio­enriched N-Acylated β-Amino Alcohols2016Inngår i: Synthesis (Stuttgart), ISSN 0039-7881, E-ISSN 1437-210X, Vol. 48, nr 19Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    Suzuki-type cross-coupling of enantiomerically enriched O-(α-bromoacyl) cyanohydrins with aromatic boronic acids substituted with electron-withdrawing or electron-donating groups gave the expected coupling products in high yields without racemization. These substrates exhibit higher reactivities than analogous substrates lacking the nitrile function, probably as a result of π-coordination of the nitrile to palladium. Reduction of the nitrile group of the products, with accompanying intramolecular acyl transfer, provides access to biologically interesting N-acylated β-amino alcohols.

  • 37.
    Izquierdo, June
    et al.
    Univ Basque Country, Dept Quim Organ 1, UPV EHU, Manuel Lardizabal 3, San Sebastian 20018, Spain..
    Demurget, Noemie
    Univ Basque Country, Dept Quim Organ 1, UPV EHU, Manuel Lardizabal 3, San Sebastian 20018, Spain..
    Landa, Aitor
    Univ Basque Country, Dept Quim Organ 1, UPV EHU, Manuel Lardizabal 3, San Sebastian 20018, Spain..
    Brinck, Tore
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Tillämpad fysikalisk kemi.
    Mercero, Jose M.
    Euskal Herriko Unibertsitatea, Kimika Fak, UPV EHU, Donostia San Sebastian, Spain.;Donostia Int Phys Ctr DIPC, Donostia San Sebastian, Spain..
    Dinér, Peter
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Oiarbide, Mikel
    Univ Basque Country, Dept Quim Organ 1, UPV EHU, Manuel Lardizabal 3, San Sebastian 20018, Spain..
    Palomo, Claudio
    Univ Basque Country, Dept Quim Organ 1, UPV EHU, Manuel Lardizabal 3, San Sebastian 20018, Spain..
    Asymmetric Synthesis of Adjacent Tri- and Tetrasubstituted Carbon Stereocenters: Organocatalytic Aldol Reaction of an Hydantoin Surrogate with Azaarene 2-Carbaldehydes2019Inngår i: Chemistry - A European Journal, ISSN 0947-6539, E-ISSN 1521-3765Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    A bifunctional amine/squaramide catalyst promoted direct aldol addition of an hydantoin surrogate to pyridine 2-carbaldehyde N-oxides to afford adducts bearing two vicinal tertiary/quaternary carbons in high diastereo- and enantioselectivity (d.r. up to >20:1; ee up to 98 %) is reported. Acid hydrolysis of adducts followed by reduction of the N-oxide group yields enantiopure carbinol-tethered quaternary hydantoin-azaarene conjugates with densely functionalized skeletons. DFT studies of the potential energy surface (B3LYP/6-31+G(d)+CPCM (dichloromethane)) of the reaction correlate the activity of different catalysts and support an intramolecular hydrogen-bond-assisted activation of the squaramide moiety in the transition state of the catalytic reaction.

  • 38.
    Josephson, Philip
    et al.
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Nykvist, Viktor
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Qasim, Wafa
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Blomkvist, Björn
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Dinér, Peter
    KTH, Skolan för kemi, bioteknologi och hälsa (CBH), Kemi, Organisk kemi.
    Student-Driven Development of Greener Chemistry in Undergraduate Teaching: Synthesis of Lidocaine Revisited2019Inngår i: Journal of Chemical Education, ISSN 0021-9584, E-ISSN 1938-1328Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    Green chemistry and sustainable development have become increasingly important topics for the education of future chemists, but the implementation of green chemistry into the chemistry curriculum requires significant efforts from teachers, especially in laboratory education. A student-driven development of a greener synthesis of Lidocaine was performed by three first-cycle, third-year students as a part of their B. Sc. degree project with the goal to implement the procedure in an under-graduate organic chemistry course. The students were merely provided with the framework for the project and were given the opportunity to independently develop the project based on an analysis of the 12 principles of green chemistry. The "greenification" of the Lidocaine synthesis by the three students led to several green improvements of the standard procedure, for example, (1) decreased reaction temperature, (2) solvent replacement, (3) fewer equivalents of the starting material (diethylamine) by the use of an inorganic bulk base, (4) use of catalytic amounts of potassium iodide to promote the Finkelstein reaction, and (5) a two-step one-pot procedure. Furthermore, one of the developed procedures was successfully implemented in a full-scale organic chemistry laboratory course.

    Fulltekst tilgjengelig fra 2020-12-01 09:46
  • 39. Klein, Michael
    et al.
    Dinér, Peter
    University of Gothenburg.
    Dorin-Semblat, Dominique
    Doerig, Christian
    Grøtli, Morten
    Synthesis of 3-(1,2,3-triazol-1-yl)- and 3-(1,2,3-triazol-4-yl)-substituted pyrazolo[3,4-d]pyrimidin-4-amines via click chemistry: potential inhibitors of the Plasmodium falciparum PfPK7 protein kinase2009Inngår i: Organic and biomolecular chemistry, ISSN 1477-0520, E-ISSN 1477-0539, Vol. 7, nr 17, s. 3421-3429Artikkel i tidsskrift (Fagfellevurdert)
  • 40. Klein, Michael
    et al.
    Krainz, Karin
    Redwan, Itedale Namro
    Dinér, Peter
    Grøtli, Morten
    Synthesis of chiral 1,4-disubstituted-1,2,3-triazole derivatives from amino acids2009Inngår i: Molecules, ISSN 1420-3049, E-ISSN 1420-3049, Vol. 14, nr 12, s. 5124-Artikkel i tidsskrift (Fagfellevurdert)
  • 41. Mesas-Sanchez, Laura
    et al.
    Diaz-Alvarez, Alba E.
    Koukal, Peter
    Dinér, Peter
    KTH, Skolan för kemivetenskap (CHE), Kemi, Organisk kemi. Uppsala University.
    Kinetic resolution of 2-hydroxy-2-aryl-ethylphosphonates by a non-enzymatic acylation catalyst2014Inngår i: Tetrahedron, ISSN 0040-4020, E-ISSN 1464-5416, Vol. 70, nr 24, s. 3807-3811Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    Optically pure hydroxyphosphonates are widely used as derivatizable compounds that can be incorporated into a variety of synthetic strategies for the preparation of other high value organic products. A non-enzymatic kinetic resolution procedure to obtain chiral 2-hydroxy-2-arylethylphosphonates from the easily available racemic counterparts is described. A range of 2-hydroxy-2-arylethylphosphonates was efficiently resolved employing a planar-chiral DMAP derived catalyst with good selectivities (up to S=68). The chiral hydroxyphosphonates were isolated in good yields and high enantiomeric excess (>94% ee).

  • 42.
    Mesas-Sanchez, Laura
    et al.
    KTH, Skolan för kemivetenskap (CHE), Kemi, Organisk kemi.
    Dinér, Peter
    KTH, Skolan för kemivetenskap (CHE), Kemi. Uppsala University, Sweden.
    A Mechanistic Investigation of the Kinetic Resolution of Secondary Aromatic Alcohols Using a Ferrocene-Based Planar Chiral 4-(Dimethylamino)pyridine Catalyst2015Inngår i: Chemistry - A European Journal, ISSN 0947-6539, E-ISSN 1521-3765, Vol. 21, nr 14, s. 5623-5631Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    A detailed computational and kinetic analysis of the acetylation of 1-phenylethanol with acetic anhydride catalyzed by planar chiral 4-(dimethylamino) pyridine (DMAP) catalyst ( )-1 is presented. The study includes a computational investigation of the potential-energy surface including the acylation and stereoselective transition states at the DFT level of theory. Experimentally, the kinetic study shows that the reaction proceeds in a first-order manner in catalyst, whereas both substrates, acetic anhydride and 1-phenylethanol, show fractional order, which is in accordance with steady-state conditions. The fractional order depends on an equilibrium between the free catalyst and the acetylated catalyst.

  • 43. Mesas-Sánchez, Laura
    et al.
    Díaz-Álvarez, Alba Estrella
    Dinér, Peter
    Uppsala University.
    Non-enzymatic kinetic resolution of 1,2-azidoalcohols using a planar-chiral DMAP derivative catalyst2013Inngår i: Tetrahedron, ISSN 0040-4020, E-ISSN 1464-5416, Vol. 69, nr 2, s. 753-757Artikkel i tidsskrift (Fagfellevurdert)
  • 44. Nielsen, M
    et al.
    Bertelsen, S
    Dinér, Peter
    Johansen, R L
    Niess, B
    Jorgensen, K A
    ORGN 703-Two diverse approaches for asymmetric organocatalytic beta-hydroxylation of alpha,beta-unsaturated electrophiles2008Inngår i: Abstracts of Papers of the American Chemical Society, American Chemical Society (ACS), 2008, Vol. 235Konferansepaper (Annet vitenskapelig)
  • 45. Nielsen, M
    et al.
    Dinér, Peter
    Jiang, H
    Zhuang, W
    Bertelsen, S
    Marigo, M
    Nielsen, J B
    Niess, B
    Jorgensen, K A
    ORGN 12-Asymmetric organocatalytic heteroatomic alpha- and beta-functionalizations of alpha,beta-unsaturated electrophiles2008Inngår i: Abstracts of Papers of the American Chemical Society, American Chemical Society (ACS), 2008, Vol. 235Konferansepaper (Annet vitenskapelig)
  • 46. Nillsson Lill, S. O.
    et al.
    Dinér, Peter
    University of Gothenburg.
    Pettersen, D.
    Amedjkouh, M.
    Ahlberg, P.
    Nilsson Lill, Sten O.
    Development of chiral catalysts for stereoselective synthesis by deprotonations: Experimentation in Interplay with Computational Chemistry2004Inngår i: Advances in Quantum Chemistry, ISSN 0065-3276, E-ISSN 2162-8815, Vol. 47, s. 1-22Artikkel i tidsskrift (Fagfellevurdert)
  • 47. Nordström, Helena
    et al.
    Winquist, Johan
    Geitmann, Matthis
    Solbak, Sara
    Homan, Evert
    Dinér, Peter
    Hämäläinen, Markku
    Danielson, Helena
    Identification of Fragments for Design of HIV-1 Protease Inhibitors with Allosteric Mechanisms and New Resistance ProfilesManuskript (preprint) (Annet vitenskapelig)
  • 48. Pettersen, D.
    et al.
    Dinér, Peter
    University of Gothenburg.
    Amedjkouh, M.
    Ahlberg, P.
    Composition and structure of activated complexes in stereoselective deprotonation of cyclohexene oxide by a mixed dimer of chiral lithium amide and lithiated imidazole2004Inngår i: Tetrahedron: asymmetry, ISSN 0957-4166, E-ISSN 1362-511X, Vol. 15, nr 10, s. 1607-1613Artikkel i tidsskrift (Fagfellevurdert)
  • 49. Poon, Jia-Fei
    et al.
    Alao, John Patrick
    Sunnerhagen, Per
    Dinér, Peter
    Uppsala University.
    Azastilbenes: a cut-off to p38 MAPK inhibitors2013Inngår i: Organic and biomolecular chemistry, ISSN 1477-0520, E-ISSN 1477-0539, Vol. 11, nr 27Artikkel i tidsskrift (Fagfellevurdert)
  • 50.
    Prathap, Kaniraj Jeya
    et al.
    KTH, Skolan för kemivetenskap (CHE), Kemi, Organisk kemi.
    Wu, Qiong
    KTH, Skolan för kemivetenskap (CHE), Fiber- och polymerteknologi.
    Olsson, Richard T.
    KTH, Skolan för kemivetenskap (CHE), Fiber- och polymerteknologi.
    Dinér, Peter
    KTH, Skolan för kemivetenskap (CHE), Kemi, Organisk kemi.
    Catalytic Reductions and Tandem Reactions of Nitro Compounds Using in Situ Prepared Nickel Boride Catalyst in Nanocellulose Solution2017Inngår i: Organic Letters, ISSN 1523-7060, E-ISSN 1523-7052, Vol. 19, nr 18, s. 4746-4749Artikkel i tidsskrift (Fagfellevurdert)
    Abstract [en]

    A mild and efficient method for the in situ reduction of a wide range of nitroarenes and aliphatic nitrocompounds to amines in excellent yields using nickel chloride/sodium borohydride in a solution of TEMPO-oxidized nanocellulose in water (0.01 wt %) is described. The nanocellulose has a stabilizing effect on the catalyst, which increases the turnover number and enables low loading of nickel catalyst (0.1-0.25 mol % NiCl2). In addition, two tandem protocols were developed in which the in situ formed amines were either Boc-protected to carbamates or further reacted with an epoxide to yield β-amino alcohols in excellent yields.

12 1 - 50 of 56
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