Synthesis and comparative anticancer studies of Novel amide functoinalised thienopyridine and pyridothienopyrimidinone derivatives

Abstract

Amide functionalized trifluoromethyl thieno[2,3-b] pyridine derivatives as a series were prepared starting from reaction between 1,3 di-ketone and thiocyanoacetamide. Compound 3 reacts with bromoethyl acetate to give compound 4. Compound 4 on reaction with diverse substituted aromatic and aliphatic amines gives amide derivatives 5a-f and these amide derivatives on reaction with triethylorthoformate give pyridothienopyrimidinone derivatives 6a-f. All the final compounds were evaluated for anti cancer activity against four human cancer cell lines such as A549—Lung cancer (CCL-185), MCF7—Breast cancer (HTB-22), DU145—Prostate cancer (HTB-81) and HeLa—Cervical cancer (CCL-2) by using MTT assay. Promising compound 5d was identified.