title: Identification of potent type I MetAPs inhibitors by simple bioisosteric replacement. Part 2: SAR studies of 5-heteroalkyl substituted TCAT derivatives.
abstract: Systematic SAR studies on the thiazole ring 5-substituent of TCAT derivatives revealed that the introduction of a beta-alkoxy or an amino group enhanced the inhibitory activity significantly. The present compounds are representative of specific Co(II)-MetAP1 inhibitors. Before the physiologically relevant metal ions for MetAPs are established, these small molecular compounds could be used as tools for detailed biological studies.
authors: Chinese National Center for Drug Screening, Shanghai Institute of Materia Medica, Shanghai Graduate School of the Chinese Academy of Sciences, Chinese Academy of Sciences, 189 Guoshoujing Road, Zhangjiang Hi-Tech Park, Shanghai 201203, PR China.
authors: Yong-Mei
authors: YM
authors: Cui
authors: Qing-Qing
authors: QQ
authors: Huang
authors: Jie
authors: J
authors: Xu
authors: Ling-Ling
authors: LL
authors: Chen
authors: Jing-Ya
authors: JY
authors: Li
authors: Qi-Zhuang
authors: QZ
authors: Ye
authors: Jia
authors: J
authors: Li
authors: Fa-Jun
authors: FJ
authors: Nan
mesh_terms: D000478:Alkylation; D000626:Aminopeptidases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D020128:Inhibitory Concentration 50; D007536:Isomerism; D063208:Methionyl Aminopeptidases; D015394:Molecular Structure; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D011480:Protease Inhibitors; D013844:Thiazoles; D000626:Aminopeptidases; D063208:Methionyl Aminopeptidases