Design, synthesis and biological evaluation of 9-aryl-5H-pyrido[4,3-b]indole derivatives as potential tubulin polymerization inhibitors.

ABSTRACT: A series of new 9-aryl-5H-pyrido[4,3-b]indole derivatives as tubulin polymerization inhibitors were designed, synthesized, and evaluated for antitumor activity. All newly prepared compounds were tested for their anti-proliferative activity in vitro against three different cancer cells (SGC-7901, HeLa, and MCF-7). Among the designed compounds, compound 7k displayed the strongest anti-proliferative activity against HeLa cells with IC₅₀ values of 8.7 ± 1.3 μM. In addition, 7k could inhibit the polymerization of tubulin and disrupt the microtubule network of cells. Further mechanism studies revealed that 7k arrested cell cycle at the G2/M phase and induced apoptosis in a dose-dependent manner. Molecular docking analysis confirmed that 7k<

SUBMITTER: Shi L 

PROVIDER: S-EPMC9520531 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature