Novel Indole-Containing Hybrids Derived from Millepachine: Synthesis, Biological Evaluation and Antitumor Mechanism Study.

ABSTRACT: Millepachine, a bioactive natural product isolated from the seeds of Millettia pachycarpa, is reported to display potential antitumor activity. In this study, novel indole-containing hybrids derived from millepachine were designed, synthesized and evaluated for their antitumor activities. Among all the compounds, compound 14b exhibited the most potent cytotoxic activity against five kinds of human cancer cell lines, with IC₅₀ values ranging from 0.022 to 0.074 μM, making it almost 100 times more active than millepachine. Valuable structure-activity relationships (SARs) were obtained. Furthermore, the mechanism studies showed that compound 14b induced cell-cycle arrest at the G2/M phase by inhibiting tubulin polymerization and further induced cell apoptosis through

SUBMITTER: Liang B 

PROVIDER: S-EPMC9921564 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature