Design, Synthesis and Evaluation of N13-Substituted Evodiamine Derivatives against Human Cancer Cell Lines

The study developed N13-substituted evodiamine derivatives to improve their anticancer properties, focusing on enhancing solubility and cytotoxicity against human cancer cell lines such as prostate, lung, breast, colon, and glioblastoma. Among the 38 synthesized derivatives, compound 2-16 showed the most significant cytotoxicity with an IC50 of less than 2 μM across all tested lines. The derivatives also induced apoptosis, with compounds 2-3 and 3-2 notably increasing early apoptosis in breast cancer cells. The research concluded that N13-position substitutions enhanced the antitumor activity and solubility of evodiamine derivatives, suggesting their potential as promising candidates for further anticancer drug development.