Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants.
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DOI: 10.1021/acs.jmedchem.8b01845
Abstract: Drug resistance due to acquired mutations that constitutively activate c-KIT is a significant challenge in the treatment of patients with gastrointestinal stromal tumors (GISTs). Herein, we identified 1-(5-ethyl-isoxazol-3-yl)-3-(4-{2-[6-(4-ethylpiperazin-1-yl)pyrimidin-4-ylamino]-thiazol-5-yl}phenyl)urea (10a) as a potent inhibitor against unactivated… read more here.
Keywords: discovery conformational; activated kit; kit; control inhibitors ... See more keywords
Conformational Control of Initiation Rate in Hoveyda–Grubbs Precatalysts
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DOI: 10.1021/acs.organomet.8b00041
Abstract: When the coordinating isopropyl ether of the Hoveyda precatalyst is replaced by a cyclohexyl ether, it is possible to control the substituent’s conformation in either the equatorial or axial position. A stereodivergent synthesis of axial… read more here.
Keywords: initiation rate; control initiation; control; hoveyda grubbs ... See more keywords
Conformational control of Pd2L4 assemblies with unsymmetrical ligands†
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DOI: 10.1039/c9sc05534g
Abstract: With increasing interest in the potential utility of metallo-supramolecular architectures for applications as diverse as catalysis and drug delivery, the ability to develop more complex assemblies is keenly sought after. Despite this, symmetrical ligands have… read more here.
Keywords: pd2l4 assemblies; metallo supramolecular; control pd2l4; pd2l4 ... See more keywords
Conformational control of N-methyl-N,N'-diacylhydrazines by noncovalent carbon bonding in solution.
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DOI: 10.1039/d0cc00943a
Abstract: In recent years, some X-ray structural and computational evidence has emerged for noncovalent carbon bonding (C-bond). However, evidence of C-bonds in solution is limited. Herein, from the conformational analyses of strategically designed N-methyl-N,N'-diacylhydrazines, we for… read more here.
Keywords: noncovalent carbon; carbon bonding; methyl diacylhydrazines; conformational control ... See more keywords