Abstract

On the pharmaceutical account of the reported anticancer activity of thieno[2,3-b] pyridine and condensed thieno[2,3-b]pyridine, new compounds containing thieno[2,3-b] pyridine condensed with each of pyridine, cyclopentyl, tetrahydroquinoline, pyrimidine, 1,6-naphthiridin, benzofuro[2,3-b]pyridine, imidazo[1,2-c] pyrimidine, [1,2,3]triazolo[1,5-a]pyrimidine were synthesized through different chemical reactions. The obtained compounds were evaluated for their in vitro antitumor activity against Liver HepG-2 and Breast MCF-7 cell lines compared to the reference drug (doxorubicin). Compounds 5, 7, 12, 23, 24, 37 and 39 were found to be the most active against both cell lines exhibiting IC₅₀ values ranging from 10.33-43.90 µM/L and 9.70-48.80 µM/L against HepG-2 and MCF-7 cell lines; respectively. From which compound 5 was the most active compound exerting comparable activity to the reference drug against both cell lines, showing IC₅₀ values 10.33 and 9.70 µM/L comparable to doxorubicin that exerted IC₅₀ values 8.55 and 8.90 µM/L against HepG-2 and MCF-7 cell lines; respectively.

Keywords: Thienopyridine, pyridothienopyridine, pyridothienopyrimidine, anticancer, liver HepG-2, breast MCF-7