Synthesis and biological activities of vitamin D-like inhibitors of CYP24 hydroxylase
نویسندگان
چکیده
منابع مشابه
synthesis and characterization of potentially biological active cyclometallated organoplatinum(ii) complexes
this work is presented in five parts. in the first part preparation of the starting complex [pt(c^n)cl(dmso)], 1, in which c^n = n(1),c(2?)-chelated, deprotonated 2-phenylpyridine, and dmso = dimethylsulfoxide, and its reaction with 1 equiv of the biphosphine ligands bis(diphenylphosphino)amine, dppa, or bis(diphenylphosphino)methane, dppm, to give the complex [pt(c^n)cl(dppa)], 2, or [pt(c^n)c...
15 صفحه اولDesign, Synthesis and Biological Evaluation of Novel Peptide-Like Analogues as Selective COX-2 Inhibitors
A new series of peptide-like derivatives containing different aromatic amino acids andpossessing pharmacophores of COX-2 inhibitors as SO2Me or N3 attached to the para positionof an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2)inhibitors. The synthetic reactions were based on the solid phase peptide synthesis methodusing Wang resin. One of the analogues, i...
متن کاملDesign, Synthesis and Biological Evaluation of Novel Peptide-Like Analogues as Selective COX-2 Inhibitors
A new series of peptide-like derivatives containing different aromatic amino acids andpossessing pharmacophores of COX-2 inhibitors as SO2Me or N3 attached to the para positionof an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2)inhibitors. The synthetic reactions were based on the solid phase peptide synthesis methodusing Wang resin. One of the analogues, i...
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کاتالیست یک سنتز جدید برای تیواترها توصیف شده است. واکنش الکل ها با آریل، هتروآریل و آلکیل تیو ل ها درحضور 1،3،5- تری آزو- 2،4،6- تری فسفرین-2،2،4،4،6،6 هگزاکلراید ((tapc به عنوان یک کاتالیست موُثر، بازده های خوب تا عالی از تیواترها را حاصل می کند. علاوه براین، واکنش تحت شرایط بدون فلز و بدون حلال پیش می رود، بنابراین یک مکمل جالب برای روش های شناخته شده سنتز تیواترها ارائه می دهد. یک مکانیسم ا...
15 صفحه اولSmall-molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): synthesis and biological evaluation.
The synthesis of imidazole styrylbenzamide, tert-butyl styrylimidazole, and tert-butyl styrylsulfonate derivatives is described. Evaluation of binding affinity and inhibitory activity against CYP24A1 identified the imidazole styrylbenzamides as potent inhibitors of CYP24A1, having selectivity with respect to CYP27B1 comparable with or greater than that of the standard ketoconazole. Further eval...
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ژورنال
عنوان ژورنال: Steroids
سال: 2012
ISSN: 0039-128X
DOI: 10.1016/j.steroids.2011.11.007