Design, synthesis, and biological evaluation of new pyrimidine-5-carbonitrile derivatives as novel anti-cancer, dual EGFR^WT/COX-2 inhibitors with docking studies

Abstract

A series of pyrimidine-5-carbonitriles was designed and synthesized as potential anti-cancer agents with dual EGFRWT/COX-2 inhibition. Compounds 4e and 4f disclosed the highest activity on all NCI60 cell lines.

Anticancer potential of novel symmetrical and asymmetrical dihydropyridines against breast cancer via EGFR inhibition: molecular design, synthesis, analysis and screening

“…The inhibitory activity of the potent compounds (HD-6, HD-7, HD-8 & lapatinib) against EGFR wt kinase was assessed using the EGFR wt Kinase Assay Kit from BPS biosciences as per the manufacturer's instructions. 42,43 To initiate the enzymatic reaction, a master mixture containing EGFR wt enzyme, substrates, ATP, and kinase assay enzymatic buffer was incubated with the tested compounds for 40 minutes at 30 °C. The reaction was halted by adding a detecting reagent (Kinase-Glo Max reagent) and further incubating at room temperature for 15 minutes.…”