5-Arylthio-Substituted 2-Amino-4-oxo-6-methylpyrrolopyrimidine Antifolates as Thymidylate Synthase Inhibitors and Antitumor Agents

Article abstract of DOI:10.1021/jm00022a015

Classical antifolate inhibitors of thymidylate synthase (TS) often require the reduced folate uptake system in order to exert their antitumor effects.In addition, these analogues are polyglutamylated via the enzyme folylpoly-γ-glutamate synthetase (FPGS),