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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Mini-Review Article

2-Substituted-mercapto-quinazolin-4(3H)-ones as DHFR Inhibitors

Author(s): Hussein I. El-Subbagh* and Mohamed A. Sabry

Volume 21, Issue 16, 2021

Published on: 03 March, 2021

Page: [2249 - 2260] Pages: 12

DOI: 10.2174/1389557521666210304105736

Price: $65


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).

Keywords: dihydrofolatereductase (DHFR) inhibitors, 2-thioxo-quinazolin-4(3H)-one, molecular docking studies, p-system, deoxy-thymidine monophosphate(dTMP), thymidylate synthase (TS).

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