Antifolates: current developments.

作者: Elizabeth A. Rayl , Giuseppe Pizzorno

DOI: 10.1007/978-1-4613-1267-3_8

关键词: MetaboliteDihydrofolate reductaseMethotrexateBiochemistryAntimetaboliteBiologyAntifolateBacteriaAntagonistEnzyme inhibitor

摘要: This group of Chemotherapic agents represents the first class antimetabolites synthesized and successfully proven to have antitumor activity. The concept antimetabolite was conceived in 1940 when Woods Fildes described activity sulfonamides on bacteria suggested that antimicrobial effect related some sort competition with normal utilization p-aminobenzoic acid, a fundamental metabolite for [1,2]. Following characterization synthesis folic acid 1946, number analogues were tested [3]. derivative x-methyl-folic which produced changes blood counts, particularly granulocytes, bone marrow rats [4]. However, this antagonist had no humans.

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