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

Hussein    I.    El-Subbagh; Mohamed    A.    Sabry

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: 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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Mini-Reviews in Medicinal Chemistry

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).

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El-Subbagh I. Hussein*, Sabry A. Mohamed , 2-Substituted-mercapto-quinazolin-4(3H)-ones as DHFR Inhibitors, Mini-Reviews in Medicinal Chemistry 2021; 21 (16) . https://dx.doi.org/10.2174/1389557521666210304105736

DOI https://dx.doi.org/10.2174/1389557521666210304105736	Print ISSN 1389-5575
Publisher Name Bentham Science Publisher	Online ISSN 1875-5607

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