Mechanism-based design, synthesis and biological studies of N 5-substituted tetrahydrofolate analogs as inhibitors of cobalamin-dependent methionine synthase and …

Z Zhang, C Tian, S Zhou, W Wang, Y Guo, J Xia…

文献索引：Zhang, Zhili; Tian, Chao; Zhou, Shouxin; Wang, Wei; Guo, Ying; Xia, Jie; Liu, Zhenming; Wang, Biao; Wang, Xiaowei; Golding, Bernard T.; Griff, Roger J.; Du, Yansheng; Liu, Junyi European Journal of Medicinal Chemistry, 2012 , vol. 58, p. 228 - 236

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被引用次数: 8

摘要

A number of 8-deazatetrahydrofolates bearing electrophilic groups on N5 were designed and synthesized based on the action mechanism of methionine synthase, and their biological activities were investigated as well. Compounds (11b, 12b and 16) showed the most active against methionine synthase (IC50: 8.11 μM, 1.73 μM, 1.43 μM). In addition, the cytotoxicity to human tumor cell lines and dihydrofolate reductase (DHFR) inhibition by ...