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- Title
Synthesis, Antifolate and Anticancer Activities of N<sup> 5</sup>-Substituted 8,10-Dideazatetrahydrofolate Analogues.
- Authors
Tian, Chao; Zhang, Zhili; Zhou, Shouxin; Yuan, Mengmeng; Wang, Xiaowei; Liu, Junyi
- Abstract
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 N10 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 BGC823 which were much better than MTX.
- Subjects
TETRAHYDROFOLATE dehydrogenase; TETRAHYDROFOLATE synthase; CANCER treatment; CANCER cell analysis; BIOLOGICAL assay; CANCER chemotherapy; METHYLATION; MASS spectrometers
- Publication
Chemical Biology & Drug Design, 2016, Vol 87, Issue 3, p444
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.12681