Novel indolyl 1,2,4-triazole derivatives as potential anti-proliferative agents: in silico studies, synthesis, and biological evaluation.

ABSTRACT: A new series of indolyl 1,2,4-triazole scaffolds was designed, synthesised, and biologically evaluated for their inhibitory activity against both CDK4 and CDK6. The results ranged from 0.049 μM to 3.031 μM on CDK4 and from 0.075 μM to 1.11 μM on CDK6 when compared to staurosporine, with IC₅₀ values of 1.027 and 0.402 μM, respectively. Moreover, all compounds were tested for their cytotoxicity against two breast cancer cell lines, MCF-7 and MDA-MB-231. All of the synthesised compounds showed promising anti-proliferative activity, with two compounds Vf (IC₅₀ = 2.91 and 1.914 μM, respectively) and Vg (IC₅₀ = 0.891 and 3.479 μM, respectively) having potent cytotoxic activity in comparison to the reference staurosporine (IC₅₀ = 3.144 and 4.385 μM, res

SUBMITTER: Ghobish SA 

PROVIDER: S-EPMC10809324 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature