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Review
. 2021;21(16):2249-2260.
doi: 10.2174/1389557521666210304105736.

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

Hussein I El-Subbagh  1 , Mohamed A Sabry  1
Affiliations
Review

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

Hussein I El-Subbagh et al. Mini Rev Med Chem. 2021.

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).

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

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