Synthesis, Antifolate and Anticancer Activities of  N   5  ‐Substituted 8,10‐Dideazatetrahydrofolate Analogues | Zendy

Tian Chao | Zendy; Zhang Zhili | Zendy; Zhou Shouxin | Zendy; Yuan Mengmeng | Zendy; Wang Xiaowei | Zendy; Liu Junyi | Zendy

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Synthesis, Antifolate and Anticancer Activities of N 5 ‐Substituted 8,10‐Dideazatetrahydrofolate Analogues

Author(s) -

Tian Chao,

Zhang Zhili,

Zhou Shouxin,

Yuan Mengmeng,

Wang Xiaowei,

Liu Junyi

Publication year - 2016

Publication title -

chemical biology and drug design

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.59

H-Index - 77

eISSN - 1747-0285

pISSN - 1747-0277

DOI - 10.1111/cbdd.12681

Subject(s) - antifolate , stereochemistry , chemistry , combinatorial chemistry , antimetabolite , organic chemistry , toxicity

Based on our previous work, seven N 5 ‐substituted 8,10‐dideazatetrahydrofolate analogues and one 8‐deazatetrahydrofolate analogue were designed and synthesized as human dihydrofolate reductase ( hDHFR ) inhibitors. All compounds were assayed versus DHFR and five different cancer cell lines. The biological assay indicated that replacing N 10 with carbon would significantly increase inhibitory activities against DHFR and cytotoxicities against cancer cell lines. Compound 19a with 4‐amino and N 5 ‐formyl showed great antitumour activities against HL ‐60, Bel‐7402 and BGC 823 which were much better than MTX .

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