Asymmetric synthesis of isobenzofuranone derivatives and their unique character as protein kinase Cα (PKCα) activators
摘要:
Efficient enantio-selective synthesis of conformationally constrained diacylglycerol analogues, 7-substituted isobenzofuranone derivatives, originally developed by us as PKC alpha ligands, was achieved by asymmetric dihydroxylation and gamma-lactone formation via ortho-lithiation and carboxylation. A series of derivatives having straight and/or branched side chains were synthesized and evaluated, and low-nanomolar-concentration affinity ligands and highly potent PKC alpha activators were found among them. These potent ligands induced phenotypic change of K562 cells, which is characteristic of PKC activators. (C) 2009 Elsevier Ltd. All rights reserved.
Regioselective hydrostannations catalyzed by molybdenum isonitrile complexes
作者:Sascha Braune、Uli Kazmaier
DOI:10.1016/s0022-328x(01)01309-2
日期:2002.1
selectivities obtained with this catalyst are significantly higher in comparison to the results obtained with the commonly used palladium and rhodium catalysts. The influence of the isonitrile incorporated into the molybdenumcomplex is investigated.
Efficient enantio-selective synthesis of conformationally constrained diacylglycerol analogues, 7-substituted isobenzofuranone derivatives, originally developed by us as PKC alpha ligands, was achieved by asymmetric dihydroxylation and gamma-lactone formation via ortho-lithiation and carboxylation. A series of derivatives having straight and/or branched side chains were synthesized and evaluated, and low-nanomolar-concentration affinity ligands and highly potent PKC alpha activators were found among them. These potent ligands induced phenotypic change of K562 cells, which is characteristic of PKC activators. (C) 2009 Elsevier Ltd. All rights reserved.