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

作者：Ghorab Mostafa M; Shaaban Mohamed A; Refaat Hanan M^*; Heiba Helmy I; Ibrahim Sara S

来源：European Journal of Medicinal Chemistry, 2012, 53: 403-407.

DOI：10.1016/j.ejmech.2012.04.009

• 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.

• 出版日期2012-7