Dwivedi, Ashish RanjanKumar, VijayYadav, Ravi PrakashKumar, NaveenJangid, KailashAnand, PiyushSharma, Deepak KumarBarnawal, SomeshKumar, Vinod2024-01-212024-08-132024-01-212024-08-132022-06-2622286010.1016/j.molstruc.2022.133592https://kr.cup.edu.in/handle/32116/3549Ligands binding to the colchicine domain of the tubulin protein act as tubulin polymerization inhibitors and arrest the cell cycle in G2/M phase. A series of 4-Phenyl-1,2,3-triazole substituted pyrimidine derivatives have been synthesized and evaluated for antiproliferative and antitubulin activities. In the series, AV-6 and AV-14 were found to be active against the three tested cancer cell lines wherein AV-6 displayed IC50 values of 1.2 �M, 5.5 �M, and 1.9 �M while AV-14 displayed IC50 values of 4.7 �M, 1.7 �M, and 1.4 �M against HCT-116, MCF-7 and HT-29 cell lines, respectively. These compounds were found to be non toxic to the normal cells (HEK-293). In the cell cycle analysis and JC-1 studies, these compounds induce mitocondria mediated apoptosis. In the tubulin polymerization inhibition studies, AV-6 displayed significant tubulin polymerization inhibition potential. In the molecular docking and simulation studies, these compounds fit well in the active site of colchicine. � 2022 Elsevier B.V.en-US4-Phenyl-1,2,3-triazolepyrimidinesAnticancerAntiproliferativeColchicine binding siteTubulin polymerization inhibitorsArticlehttps://linkinghub.elsevier.com/retrieve/pii/S0022286022012480