期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 58, 期 -, 页码 228-236出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.09.027
关键词
8-Deazatetrahydrofolates; Antitumor; Methionine synthase; Folate inhibitor
资金
- National Science Foundation of China [20972011, 21042009, 21172014]
- Ministry of Science and Technology of China [2009ZX09301-010]
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.
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