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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.

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