A series of 2,4-diaminopyrimidine-5-carbonitrile and N-(2-amino-5-cyanopyrimidin-4-yl) benzamide derivatives (5–14) were synthesized and their chemical structures were confirmed by 1 H, 13C NMR and mass spectral data. Anticancer activity of all the synthesized compounds were evaluated for in vitro cytotoxic activity against a panel of four human cancer cell lines i.e., human breast (MCF-7,), cervical cancer (C33A), oral (KB) and prostrate (DU-145). All the examined compounds, demonstrated potent to moderate anticancer activity. Among all the synthesized compounds, 6 and 11 were exhibited more potent activity. Docking studies for 6 and 11 into EGFR active site was carried out to investigate their potential binding modes. Therefore, compounds 6 and 11 can be considered as fascinating candidates for further expansion of more potent anticancer agents.
Ismail, P. S., Khan, I., Kumar, V., Verma, V. P., Shukla, M., Dhasmana, A., Pandey, S., Pal Singh, G., Khan, S., & Singh, J. (2019). Synthesis and biological evaluation of 2,4-diaminopyrimidine-5-carbonitrile and N-(2-amino-5-cyanopyrimidin-4-yl)benzamide derivatives as EGFR inhibitors. Chemistry & Biology Interface, 9(33), 148–156.
Chemistry & Biology Interface
Immunology and Microbiology