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Updated: Nov 15, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
2-Substituted-mercapto-quinazolin-4(3H)-ones as DHFR Inhibitors
Hussein I El-Subbagh1, Mohamed A Sabry1
1Department of Medicinal Chemistry, College of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
Abstract:
Antifolates are a class of drugs used as antibacterial, antiparasitic, and anticancer agents. This review focuses on 2-substituted-mercapto-quinazolin-4(3H)-one analogues as dihydrofolatereductase (DHFR) inhibitors. Several research work have concluded a structural model for this class of 2-thio-quinazoline derivatives to get compounds with remarkable biological activity. The pattern and orientation of the p-system substitutions with regard to the quinazoline nucleus manipulate the activity. The application of the obtained model criteria produced compounds 18, 20 and 21, which proved to be 4-8 times more active than the reference drug methotrexate (MTX, 1).
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