Identification of potent type I MetAPs inhibitors by simple bioisosteric replacement. Part 2: SAR studies of 5-heteroalkyl substituted TCAT derivatives |
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| Authors: | Cui Yong-Mei Huang Qing-Qing Xu Jie Chen Ling-Ling Li Jing-Ya Ye Qi-Zhuang Li Jia Nan Fa-Jun |
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| Affiliation: | 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. |
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| 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. |
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