Colorectal anticancer activity of a novel class of triazolic triarylmethane derivatives.

ABSTRACT: 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 showe

SUBMITTER: Hadj Mohamed A 

PROVIDER: S-EPMC10880923 | biostudies-literature | 2024 Feb

REPOSITORIES: biostudies-literature