Development of di-arylated 1,2,4-triazole-based derivatives as therapeutic agents against breast cancer: synthesis and biological evaluation.

ABSTRACT: The synthesis, anticancer activity, and metabolic stability of di-arylated 1,2,4-triazole molecules have been reported. Utilizing an efficient programmed arylation technique which starts from commercially available 3-bromo-1H-1,2,4-triazole, a series of therapeutic agents have been synthesized and screened against three human breast cancer cell lines, MDA-MB-231, MCF-7, and ZR-75-1, via an in vitro growth inhibition assay. At 10 μM concentration, 4k, 4m, 4q, and 4t have displayed good anticancer potency in the MCF-7 cell line, among which 4q has shown the best efficacy (IC₅₀ = 4.8 μM). Mechanistic investigations of 4q have indicated the elevation of the pro-apoptotic BAX protein in the malignant cells along with mitochondrial outer membrane permeabilization

SUBMITTER: Deb M 

PROVIDER: S-EPMC11411613 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature