NOVEL PYRROLOPYRIMIDINES AND TRIAZOLOPYRROLOPYRIMIDINES CARRYING A BIOLOGICALLY ACTIVE SULFONAMIDE MOIETIES AS ANTICANCER AGENTS

作者：Ghorab Mostafa M^*; Alsaisd Mansour S; Nissan Yassin M

来源：Acta Poloniae Pharmaceutica, 2015, 72(1): 65-78.

• anticancer
• pyrrolopyrimidines
• triazolopyrrolopyrimidines
• sulfonamides

A new series of pyrroles 5, 6, pyrrolopyrimidines 8, 11-14, 16-29, triazolo-pyrrolopyrimidines 9, 10 and 15 carrying a biologically active sulfonamide moities wee synthesized using 2-amino-3-cyano-4-(4-bromophenyl)pyrrole 5 as a strategic starting material. The structures of the prepared compounds were confirmed by elemental analyses, IR, H-1-NMR and C-13-NMR data. All of the synthesized compounds showed promising anticancer activity against breast cancer cell line (MCF7) compared to doxorubicin as reference drug, especially compounds 5-17, 21-24 and 28 with better IC50 than that of doxorubicin. In order to suggest the mechanism of action of their cytotoxic activities, molecular docking on the active site of c-Src was done and good results were obtained.

• 出版日期2015-2