title: Anticancer and radiosensitizing evaluation of some new pyranothiazole-Schiff bases bearing the biologically active sulfonamide moiety.
abstract: 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 (IC(50): 27.51, 10.25, 9.55, 9.39 and 9.70 μM, respectively) exhibited higher cytotoxic activities than the reference drug doxorubicin (IC(50): 32.00 μM). Additionally, the previously mentioned compounds were evaluated again for their ability to enhance the cell killing effect of γ-radiation.
authors.affiliation: Medicinal, Aromatic and Poisonous Plants Research Center, College of Pharmacy, King Saud University, PO Box 2457, Riyadh 11451, Saudi Arabia.
authors.forename: Mostafa M
authors.initials: MM
authors.lastname: Ghorab
authors.forename: Mohamed A
authors.initials: MA
authors.lastname: Shaaban
authors.forename: Hanan M
authors.initials: HM
authors.lastname: Refaat
authors.forename: Helmy I
authors.initials: HI
authors.lastname: Heiba
authors.forename: Sara S
authors.initials: SS
authors.lastname: Ibrahim
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects / Q000528:radiation effects; D015195:Drug Design; D005720:Gamma Rays; D006801:Humans; D020128:Inhibitory Concentration 50; D011838:Radiation-Sensitizing Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D012545:Schiff Bases / Q000737:chemistry; D013449:Sulfonamides / Q000737:chemistry*; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011838:Radiation-Sensitizing Agents; D012545:Schiff Bases; D013449:Sulfonamides; D013844:Thiazoles