Design, synthesis, and biological evaluation of novel 3-aryl-4-(3,4,5-trimethoxyphenyl)selenophene derivatives as new tubulin inhibitors.

ABSTRACT: Microtubules, composed of tubulin subunits, represent a critical target in anticancer drug discovery. The design and evaluation of small-molecule inhibitors targeting tubulin polymerisation continue to hold significant promise for advancing cancer therapeutics. Based on structural insights into tubulin polymerisation inhibitors and tubulin interaction models, a novel series of 3-aryl-4-(3,4,5-trimethoxyphenyl)selenophene derivatives were designed as potential tubulin polymerisation inhibitors. Among the synthesised analogs, compound 7i, featuring a selenophene linker, demonstrated superior antiproliferative activity against Huh7, MCF-7, and SGC-7901 cancer cell lines, with IC₅₀ values slightly lower than those of combretastatin A-4 (CA-4). Structure-activity relationship

SUBMITTER: Xu W 

PROVIDER: S-EPMC12671418 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature