Figure 1.
Structures for classical antifolates and novel pyrrolo- and thieno[2,3-d]pyrimidine antifolates. Compounds 4–8 were previously described12–14. MTX is a dihydrofolate reductase inhibitor, whereas PMX and RTX are primarily thymidylate synthase inhibitors. Compound 9 is a novel antifolate and dihydrofolate reductase inhibitor16 that is an active and highly selective substrate for RFC over PCFT6,15.
