A series of triaminotriazine derivatives (compounds 5a–f, 6a–x, and 7a–g) was designed, synthesized, and evaluated for their inhibition activities to colorectal cancer (CRC) cell lines (HCT-116 and HT-29). Most of the synthesized compounds demonstrated moderate anti- proliferatory effects on both HCT-116 and HT-29 cell lines at the concentration of 10μM. The inhibitory activities against HCT-116 and HT-29 cell lines were discussed to develop the ...