Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives

► We discovered novel Piperazinylpyrimidine derivatives as antitumor agents. ► 4 and 15 are selective cytostatic and 16 is global cytotoxic against NCI-60 panel. ► 15 is a promising preclinical candidate investigated against in vivo models. ► 4 and 15 selectively inhibits the growth of basal-like breast cancer cell lines. ► 4, 15, and 16 are selective binders and/or inhibitors of certain kinase subfamilies