Synthesis and in vitro anticancer screening of some novel 4-[2-amino-3-cyano-4-substituted-5,6,7,8-tetrahydroquinolin-1-(4H)-yl]benzenesulfonamides

被引：44

作者：

Al-Said, Mansour S. ^{[1
]}

Ghorab, Mostafa M. ^{[1
]}

Al-qasoumi, Saleh I. ^{[2
]}

El-Hossary, Ebaa M. ^{[3
]}

Noaman, Eman ^{[4
]}

机构：

[1] King Saud Univ, Coll Pharm, MAPPRC, Riyadh 11451, Saudi Arabia

[2] King Saud Univ, Coll Pharm, Dept Pharmacognosy, Riyadh 11451, Saudi Arabia

[3] Atom Energy Author, Natl Ctr Radiat Res & Technol, Dept Drug Radiat Res, Cairo, Egypt

[4] Atom Energy Author, Natl Ctr Radiat Res & Technol, Dept Radiat Biol, Nasr City, Cairo, Egypt

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 07期

关键词：

Synthesis; quinoline; Sulfonamide; Carbonic anhydrase II; Anticancer activity; CARBONIC-ANHYDRASE INHIBITORS; RADIOPROTECTIVE AGENTS; THERAPEUTIC APPLICATIONS; SELECTIVE INHIBITORS; SULFONAMIDE MOIETY; ISOZYME-IX; ANTITUMOR; DESIGN; QUINOLINES; BEARING;

D O I：

10.1016/j.ejmech.2010.03.030

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

It has been reported that aryl/heteroaryl sulfonamide compounds may act as anticancer agents through a variety of mechanisms and the most prominent of these mechanisms is through the inhibition of carbonic anhydrase isozymes. The present work reports the possible utility of 4-(cyclohexenylamino) benzenesulfonamide in the synthesis of some novel 4-(quinolin-1-yl)benzenesulfonamide derivatives 6a-u. The structures of these compounds were confirmed by elemental analyses, IR, (1)H NMR and mass spectral data. All the newly synthesized compounds were evaluated for their in vitro anticancer activity. Some compounds showed interesting in vitro anticancer activities when compared with doxorubicin as a reference drug. In addition, docking of the synthesized compounds into carbonic anhydrase isozyme II (CA II) active site was performed in order to give a suggestion about the proposed mechanism of action. (c) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：3011 / 3018

页数：8

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