Quinazoline antifolate thymidylate synthase inhibitors: heterocyclic benzoyl ring modifications

PR Marsham, LR Hughes, AL Jackman…

Index: Marsham, Peter R.; Hughes, Leslie R.; Jackman, Ann L.; Hayter, Anthony J.; Oldfield, John; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 5 p. 1594 - 1605

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Citation Number: 100

Abstract

The principle of effective antitumor chemotherapy with a specific inhibitor of the enzyme thymidylate synthase (TS, EC 2.1. 1.45) was established in clinical of the quinazoline-based antifolate Wo-propargyl-5, 8-dideazafolic acid (l). 4-5 The unacceptable hepatic and renal toxicities