Synthesis and Biological Evaluation of Thieno[2, 3‐ d ]pyrimidine‐amides as Potential Anticancer Agents

In our search towards the development of potential anticancer agents, a new class of N ‐(3‐(thieno[2, 3‐ d ]pyrimidin‐4‐ylamino)phenyl)amides ( 10 a−x ) were synthesized and examined for their anticancer activity towards different human cancer cell lines. Of the derivatives tested, 10 g , 10 p and 10 w displayed potent growth inhibition on some of the cell lines, peculiarly 10 w exhibited selective and promising activity on MDA‐MB‐453 and MCF‐7 cell lines. In comparison to the standard ZSTK474, nearly 3 fold growth inhibitory effect was noticed with 10 w against MCF‐7 cell line. Notably, the morphology and long term clonogenic survival of MCF‐7 cells were affected by compound 10 w . Moreover, the results from AO/EB and DAPI staining studies as well as analysis of mitochondrial membrane potential divulged that the growth of MCF‐7 cells was inhibited by 10 w through the induction of apoptosis. From flow‐cytometry analysis, it is notable that 10 w shows G0/G1 cell cycle arrest in MCF‐7 cells. Overall, compound 10 w could be considered as a promising lead for the further exploration and identification of thieno[2, 3‐ d ]pyrimidine‐based anticancer agents.