期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 53, 期 -, 页码 403-407出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.04.009
关键词
Pyranothiazole; Sulfonamides; Carbonic anhydrase inhibitors; Cytotoxicity; Radiosensitizing activities
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.
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