Receptor-based design of novel dihydrofolate reductase inhibitors: Benzimidazole and indole derivatives

Article abstract of DOI:10.1021/jm00108a022

Although many thousands of inhibitors of the enzyme dihydrofolate reductase (DHFR) have been synthesized, all of the very active compounds have been 2,4-diaminopyrimidines or very close analogues. This paper describes 2,4-diamino-6-benzylbenzimidazole (3b