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Article

Substituted Quinazolines, 1. Synthesis and Antitumor Activity of Certain Substituted 2-Mercapto-4(3H)-quinazolinone Analogs

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh-11451 Saudi Arabia
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2001, 69(4), 351-366; https://doi.org/10.3797/scipharm.aut-01-205
Submission received: 5 January 2001 / Accepted: 1 June 2001 / Published: 28 December 2001

Abstract

A new series of 4(3H)-quinazolinone analogs bearing 6-iodo and 2-thioether functions were synthesized and screened for their in vitro antitumor activity. Eight compounds were identified as active anticancer agents. 2-Mercapto-3-benzyl-4-thioxo-6-iodo-3H-quinazolin (2) and 2-(2,4-dinitrophenyl)-3-benzyl-6-iodo-4-(3H)-quinazolinone(9) proved to be the most active compounds in this study. They showed MG-MID GI50, TGI, LC50 values of 3.9, 25.2, 82.3 and 2.7, 12.3, 38.7 μM, respectively. The detailed synthesis and biological screening data are reported.
Keywords: Synthesis; 4(3H)-quinazolinone; Antitumor testing Synthesis; 4(3H)-quinazolinone; Antitumor testing

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MDPI and ACS Style

Abdel Hamid, S.G.; El-Obeid, H.A.; Al-Rashood, K.A.; Khalil, A.A.; El-Subbagh, H.I. Substituted Quinazolines, 1. Synthesis and Antitumor Activity of Certain Substituted 2-Mercapto-4(3H)-quinazolinone Analogs. Sci. Pharm. 2001, 69, 351-366. https://doi.org/10.3797/scipharm.aut-01-205

AMA Style

Abdel Hamid SG, El-Obeid HA, Al-Rashood KA, Khalil AA, El-Subbagh HI. Substituted Quinazolines, 1. Synthesis and Antitumor Activity of Certain Substituted 2-Mercapto-4(3H)-quinazolinone Analogs. Scientia Pharmaceutica. 2001; 69(4):351-366. https://doi.org/10.3797/scipharm.aut-01-205

Chicago/Turabian Style

Abdel Hamid, S. G., H. A. El-Obeid, K. A. Al-Rashood, A. A. Khalil, and H. I. El-Subbagh. 2001. "Substituted Quinazolines, 1. Synthesis and Antitumor Activity of Certain Substituted 2-Mercapto-4(3H)-quinazolinone Analogs" Scientia Pharmaceutica 69, no. 4: 351-366. https://doi.org/10.3797/scipharm.aut-01-205

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