Synthesis and apoptosis inducing ability of new anilino substituted pyrimidine sulfonamides as potential anticancer agents

A series of anilino substituted pyrimidine sulfonamides were prepared and evaluated for their anticancer activity. These sulfonamides showed promising activity with IC50 values ranging from 5.6 to 12.3 μM. The detailed biological aspects of some of the promising compounds (3d, 3e and 3g) on the K562 cell line were studied. Interestingly, compounds induced G1 cell cycle arrest and down regulation of G1 phase cell cycle regulatory proteins such as cyclin D1, CDK4. These compounds also exhibited inhibition of NF-κB as well as its downstream target gene Akt1 and the phosphorylated form of AKt ser 474 proteins. One of the representative compound 3e could be considered as the potential lead for its development as a new anticancer agent.

Graphical abstractNew class of anilino substituted pyrimidine sulfonamides has been prepared and evaluated for their anticancer activity. Further, some of the biological assays related to mechanism aspects have also been carried out.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► G1 arrest in K562 cell lines. ► Population in sub-G1 indicating sulphonamides having apoptosis inducing ability. ► G1 arrest associated with cyclins and CDKs. ► Down regulation of NF-κB, Akt and STAT was also observed.