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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.
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
Print publication date: 01/12/2012
ISSN (print): 0223-5234
ISSN (electronic): 1768-3254
Publisher: Elsevier Masson
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