Design, synthesis and antiproliferative screening of newly synthesized coumarin-acrylamide hybrids as potential cytotoxic and apoptosis inducing agents.

ABSTRACT: On the basis of the observed biological activity of coumarin and acrylamide derivatives, a new set of coumarin-acrylamide-CA-4 hybrids was designed and synthesized. These compounds were investigated for their cytotoxic activity against cancerous human liver cell line HepG2 cells using 5-fluorouracil (5-FU) as a reference drug. Compound 6e had promising antiproliferative activity with an IC₅₀ value of 1.88 μM against HepG2 cells compared to 5-FU (IC₅₀ = 7.18 μM). The results of β-tubulin polymerization inhibition indicated that coumarin-acrylamide derivative 6e was the most active, with a percentage inhibition value of 84.34% compared to podophyllotoxin (88.19% β-tubulin inhibition). Moreover, the active coumarin-acrylamide molecule 6e exerted cell cycle cession at the

SUBMITTER: Abd El-Lateef HM 

PROVIDER: S-EPMC10626558 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature