Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives
文献类型:期刊论文
作者 | Cui, YM; Huang, QQ; Xu, J; Chen, LL; Li, JY![]() ![]() ![]() |
刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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出版日期 | 2005-08-15 |
卷号 | 15期号:16页码:3732-3736 |
ISSN号 | 0960-894X |
DOI | 10.1016/j.bmcl.2005.05.055 |
文献子类 | Article |
英文摘要 | A series of thiazole-4-carboxylic acid thiazol-2-ylamide (TCAT, 4) derivatives were designed and synthesized according to simple bioisosteric replacement from previously reported pyridine-2-carboxylic acid thiazol-2-ylamide (PCAT) MetAP inhibitors. The preliminary SAR studies demonstrated that these TCAT series of compounds showed different activity and selectivity compared with those of the corresponding PCAT compounds. These findings provide useful information for the design and discovery of more potent inhibitors of type I MetAPs. (c) 2005 Elsevier Ltd. All rights reserved. |
WOS关键词 | COLI METHIONINE AMINOPEPTIDASE ; ESCHERICHIA-COLI ; SACCHAROMYCES-CEREVISIAE ; FUMAGILLIN ; GENE |
WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
语种 | 英语 |
WOS记录号 | WOS:000231185800018 |
出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
源URL | [http://119.78.100.183/handle/2S10ELR8/273817] ![]() |
专题 | 国家新药筛选中心 |
通讯作者 | Li, J |
作者单位 | 1.Chinese Acad Sci, Grad Sch, Shanghai Inst Biol Sci, Shanghai Inst Mat Medcia,Chinese Natl Ctr Durg Sc, Shanghai 201203, Peoples R China 2.Univ Kansas, High Throughput Screening Lab, Lawrence, KS 66047 USA |
推荐引用方式 GB/T 7714 | Cui, YM,Huang, QQ,Xu, J,et al. Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2005,15(16):3732-3736. |
APA | Cui, YM.,Huang, QQ.,Xu, J.,Chen, LL.,Li, JY.,...&Nan, FJ.(2005).Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,15(16),3732-3736. |
MLA | Cui, YM,et al."Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 15.16(2005):3732-3736. |
入库方式: OAI收割
来源:上海药物研究所
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