5, 10-Methylenetetrahydro-5-deazafolic acid and analogs: Synthesis and biological activities

A Gangjee, J Patel, RL Kisliuk…

文献索引：Gangjee, Aleem; Patel, Jasmin; Kisliuk, Roy L.; Gaumont, Yvette Journal of Medicinal Chemistry, 1992 , vol. 35, # 20 p. 3678 - 3685

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被引用次数: 6

摘要

The synthesis of 5, 10-methylene-5-deazatetrahydrofolic acid (2), a stable, rigid analogue of 5, lO-methylenetetrahydrofolate (l), is reported as a potential inhibitor of thymidylate synthase. The target compound was obtained by a Fisher-indole type cyclization of the hydrazone 16 from 2-amino-6-hydrazino-4-oxopyrimidine (10) and diethylN-[4-(3-formyl-l- pyrrolyl) benzoyll-~-glutamate (15) followed by catalytic reduction of the product 17. ...