Substituted quinazolines, Part 2.: Synthesis and in-vitro anticancer evaluation of new 2-substituted mercapto-3H-quinazoline analogs

被引：53

作者：

Khalil, AA ^{[1
]}

Hamide, SGA ^{[1
]}

Al-Obaid, AM ^{[1
]}

El-Subbagh, HI ^{[1
]}

机构：

[1] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia

来源：

ARCHIV DER PHARMAZIE | 2003年 / 336卷 / 02期

关键词：

synthesis; 4-(3H)-quinazolinone; antitumor activity;

D O I：

10.1002/ardp.200390011

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of 2-substituted mercapto-3H-quinozolines bearing 6-iodo and 2-heteroarylthio functions was synthesized and screened for their in vitro antitumor activity Eighteen compounds were identified as active anticancer agents. N'-[(3-Benzyl-4-oxo-6-iodo-3H-quinazoline-2-yl)thioacetyl]-N-3-ethylthiosemicarbazide (10), N-benzoyl-N'-[2-(3-benzyl-4-oxo-6-iodo-3H-quinozolin-2-yl)thioacetyl]hydrazine (12), and 2-[(3,6-dioxo-pyridazin-4-yl)thio]-3-benzyl-4-oxo-6-iodo-3H-quinazoline (20) proved to be the most active members in this study. They showed MG-MID, GI(50) values of 12.8,11.3, and 13.8 muM, respectively. The detailed synthesis and biological screening data are reported.

引用

页码：95 / 103

页数：9

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