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

Lookup NU author(s): Emeritus Professor Bernard Golding, Professor Roger Griffin


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A number of 8-deazatetrahydrofolates bearing electrophilic groups on N-5 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 mu M, 1.73 mu M, 1.43 mu M). In addition, the cytotoxicity to human tumor cell lines and dihydrofolate reductase (DHFR) inhibition by target compounds were evaluated. (C) 2012 Elsevier Masson SAS. All rights reserved.

Publication metadata

Author(s): Zhang ZL, Tian C, Zhou SX, Wang W, Guo Y, Xia J, Liu ZM, Wang BA, Wang XW, Golding BT, Griffin RJ, Du YS, Liu JY

Publication type: Article

Publication status: Published

Journal: European Journal of Medicinal Chemistry

Year: 2012

Volume: 58

Pages: 228-236

Print publication date: 01/12/2012

ISSN (print): 0223-5234

ISSN (electronic): 1768-3254

Publisher: Elsevier Masson


DOI: 10.1016/j.ejmech.2012.09.027


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Funder referenceFunder name
20972011National Science Foundation of China
21042009National Science Foundation of China
21172014National Science Foundation of China
2009ZX09301-010Ministry of Science and Technology of China