Title:2-Substituted-mercapto-quinazolin-4(3H)-ones as DHFR Inhibitors
Volume: 21
Issue: 16
Author(s): Hussein I. El-Subbagh*Mohamed A. Sabry
Affiliation:
- Department of Medicinal Chemistry, College of Pharmacy, Mansoura University, Mansoura 35516,Egypt
Keywords:
dihydrofolatereductase (DHFR) inhibitors, 2-thioxo-quinazolin-4(3H)-one, molecular docking studies, p-system,
deoxy-thymidine monophosphate(dTMP), thymidylate synthase (TS).
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).
