Quinoline antifolate thymidylate synthase inhibitors: Variation of the C2- and C4-substituents

Article abstract of DOI:10.1021/jm00093a007

Modifications to the bicyclic ring system of the potent thymidylate synthase (TS) inhibitor N-[4-[N-[(2-amino-3,4-dihydro-4-oxo-6- quinazolinyl)methyl]-N-prop-2-ynylamino]benzoyl]-L-glutamic acid (1, CB3717) have led to the synthesis of a series of quinol