biostudies-literatureHadj Mohamed ACampus FranceMinistère de l’Enseignement Supérieur et de la Recherche Scientifique660-676https://www.ebi.ac.uk/biostudies/studies/S-EPMC10880923biostudies-literatureUnknown15(2)Triarylmethanes and triazoles constitute privileged structures extensively used in drug discovery programs. In this work, 12 novel triarylmethanes linked to a triazole ring were designed, synthesized, and chemically characterized aiming to target colorectal cancer. The synthetic strategy for triarylmethanes mono- and bi-substituted by a functionalized triazole ring involved a 1,3-dipolar cycloaddition. A preliminary screening in human colorectal cancer cells (HT-29 and HCT116) and murine primary fibroblasts (L929) allowed the selection of the best candidate 9b based on its high inhibition of cancer cell proliferation with an IC₅₀ of 11 μM on HT-29 and 14 μM on HCT116 and its non-cytotoxic effects on murine fibroblasts (<100 μM). A deep mechanistic study on various pathways showeRSC medicinal chemistryColorectal anticancer activity of a novel class of triazolic triarylmethane derivatives.PMC10880923PhD scholarship 964896H (2019–20)UTIQUE 2017 37094WEiffel programPHC ProgramMsaddek MHadj Mohamed ALagarde NPinon ARicco CGoya-Jorge ELiagre BMouhsine HVeitia MSfalseColorectal anticancer activity of a novel class of triazolic triarylmethane derivatives.Triarylmethanes and triazoles constitute privileged structures extensively used in drug discovery programs. In this work, 12 novel triarylmethanes linked to a triazole ring were designed, synthesized, and chemically characterized aiming to target colorectal cancer. The synthetic strategy for triarylmethanes mono- and bi-substituted by a functionalized triazole ring involved a 1,3-dipolar cycloaddition. A preliminary screening in human colorectal cancer cells (HT-29 and HCT116) and murine primary fibroblasts (L929) allowed the selection of the best candidate 9b based on its high inhibition of cancer cell proliferation with an IC₅₀ of 11 μM on HT-29 and 14 μM on HCT116 and its non-cytotoxic effects on murine fibroblasts (<100 μM). A deep mechanistic study on various pathways showe2024-01-01T00:00:00Z2024 Feb2026-06-03T00:59:42.062Z2025-04-06T22:29:55.526ZS-EPMC108809233838989110.1039/d3md00467h