Discovery and Structural Modification of Inhibitors of Methionine Aminopeptidases from Escherichia c oli and Saccharomyces c erevisiae

…, J Li, Z Qian, Q Shen, Y Li, GH Lushington…

文献索引：Luo, Qun-Li; Li, Jing-Ya; Liu, Zhi-Ying; Chen, Ling-Ling; Li, Jia; Qian, Zhen; Shen, Qiang; Li, Yu; Lushington, Gerald H.; Ye, Qi-Zhuang; Nan, Fa-Jun Journal of Medicinal Chemistry, 2003 , vol. 46, # 13 p. 2631 - 2640

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被引用次数: 60

摘要

A series of pyridine-2-carboxylic acid derivatives were synthesized according to the leads from the screening, and potent inhibitors have been obtained by structural modification. They have shown submicromolar inhibition of the enzymes (for example, for 9n, IC50= 130 nM for EcMetAP1 and IC50= 380 nM for ScMetAP1). They represent small-molecule MetAP inhibitors with novel structures different from alkylating fumagillin derivatives and peptidic ...