Design, synthesis, and anticancer activity of novel 4,6-dimorpholinyl-1,3,5-triazine compounds

Abstract A series of novel 4,6-dimorpholinyl-1,3,5-triazine derivatives 6a–6r were obtained through N-substitution and Claisen-Schmidt condensation. 1H NMR, 13C NMR, and mass spectrometry were used to characterize the molecular structures of the derivatives. The in vitro antiproliferation activity of derivatives was evaluated using the MTT assay against SW620 (human colon cancer cells), A549 (human nonsmall cell lung cancer cells), HeLa (human cervical cancer cells), and MCF-7 (human breast cancer cells). Compound 6o bearing a pyridyl group exhibited good cytotoxicity against four cancer cells, with IC50 values of 8.71, 9.55, 15.67, and 21.77 μM, sequentially. In addition, compound 6a showed some selectivity against SW620. Graphical abstract The chalcone structure was introduced into the 4,6-dimorpholinyl-1,3,5-triazine molecule through the C-N bond, and a series of new compounds were obtained. Among them, the pyridyl-containing 6o exhibits anti-proliferation activity similar to that of cisplatin on SW620. Interestingly, the phenyl-containing 6a exhibits a certain selectivity for the anti-proliferation activity of SW620.