Angiogenesis, Anti-Tumor, and Anti-Metastatic Activity of Novel α-Substituted Hetero-Aromatic Chalcone Hybrids as Inhibitors of Microtubule Polymerization.

ABSTRACT: A library of new heteroaromatic ring-linked chalcone analogs were designed and synthesized of these, compound 7m with α-CH₃ substitution and bearing a benzofuran ring, displaying the most potent activity, with IC₅₀ values of 0.07-0.183 µM against three cancer cells. Its low cytotoxicity toward normal human cells and strong potency on drug-resistant cells revealed the possibility for cancer therapy. It also could moderately inhibit in vitro tubulin polymerization with an IC₅₀ value of 12.23 µM, and the disruption of cellular architecture in MCF-7 cells was observed by an immunofluorescence assay. Cellular-based mechanism studies elucidated that 7m arrested the cell cycle at the G2/M phase and induced apoptosis by regulating the expression levels of ca

SUBMITTER: Sun M 

PROVIDER: S-EPMC8652888 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature