Methotrexate analogs. 9. Synthesis and biological properties of some 8-alkyl-7,8-dihydro analogs

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Abstract
A series of 8-alkyl-7,8-dihydromethotrexate analogs was prepared by direct alkylation of 7,8-dihydromethotrexate, after pilot studies were performed with simpler pteridines. These compounds were tested for in vitro inhibitory activity against Lactobacillus casei and as enzyme inhibitors against dihydrofolate reductase and thymidylate synthetase derived from this organism. All of the analogs were less inhibitory toward dihydrofolate reductase than was methotrexate but were more inhibitory toward thymidylate synthetase. The analogs were also evaluated for in vitro inhibitory activity against the CCRF-CEM human lymphoblastic leukemia cells. In vivo against the L1210 leukemia in mice, several of the analogs exhibited some antileukemic activity.

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