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Molecular Pharmacology, Vol 6, 573-575, Copyright © 1970 by the American Society for Pharmacology and Experimental Therapeutics

2-Amino-4-hydroxyquinazolines as Inhibitors of Thymidylate Synthetase

ORSON D. BIRD 1, JOHN W. VAITKUS 1, and JANE CLARKE 1

1 Chemistry Department, Medical and Scientific Affairs Division, Parke, Davis and Company, Ann Arbor, Michigan 48106

This paper describes a 2-amino-4-hydroxyquinazoline analogue of folic acid which is much stronger than methotrexate as a thymidylate synthetase inhibitor but weaker as a dihydrofolate reductase inhibitor. It also identifies the requirements of certain structural moieties for this activity.

Submitted on April 6, 1970






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