Anticancer and radiosensitizing evaluation of some new pyranothiazole-Schiff bases bearing the biologically active sulfonamide moiety

被引：36

作者：

Ghorab, Mostafa M. ^{[2
]}

Shaaban, Mohamed A. ^{[1
]}

Refaat, Hanan M. ^{[1
]}

Heiba, Helmy I. ^{[3
]}

Ibrahim, Sara S. ^{[3
]}

机构：

[1] Cairo Univ, Dept Organ Chem, Fac Pharm, Cairo 11562, Egypt

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

[3] Natl Ctr Radiat Res & Technol, Dept Drug Radiat Res, Nasr City, Cairo, Egypt

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 53卷

关键词：

Pyranothiazole; Sulfonamides; Carbonic anhydrase inhibitors; Cytotoxicity; Radiosensitizing activities; CARBONIC-ANHYDRASE INHIBITORS; CYTOSOLIC ISOZYME-I; THERAPEUTIC APPLICATIONS; ANTITUMOR; DERIVATIVES; TRANSMEMBRANE; AGENT; XII;

D O I：

10.1016/j.ejmech.2012.04.009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The present work reports the synthesis of some new Schiff bases, 5-(substituted benzylideneamino)-6-cyano-7H-7-(4-methoxyphenyl)-2-(4-sulphamoylphenylamino) pyrano[2,3-d]thiazole (5-15). The design of the structures of these compounds complies with the general pharmacophoric requirements for CA inhibiting anticancer drugs. The newly synthesized compounds were evaluated for their in vitro anticancer activity against human breast cancer cell line (MCF7). Most of the screened compounds showed interesting cytotoxic activities compared to doxorubicin as a reference drug. Compounds 4, 6-8 and 11 (IC50: 27.51, 10.25, 9.55, 9.39 and 9.70 mu M, respectively) exhibited higher cytotoxic activities than the reference drug doxorubicin (IC50: 32.00 mu M). Additionally, the previously mentioned compounds were evaluated again for their ability to enhance the cell killing effect of gamma-radiation. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：403 / 407

页数：5

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