Synthesis and anti-cancer biological evaluation of a novel protoapigenone analogue, WYC-241.

ABSTRACT: Natural products are an important source for developing anti-cancer agents. Previously, we identified the anti-cancer flavonoid protoapigenone from Thelypteris torresiana (Gaud.) and synthesized its derivative, WYC-0209, with improved anti-cancer properties. In this study, to further optimize this protoapigenone derivative for better therapeutic efficacy, various functional groups were introduced onto its naphthalene ring, and their anti-cancer properties were evaluated. A total of eighteen WYC-0209 derivatives were synthesized, among which the derivative containing two units of the isopentyl-substituted side chain exhibited superior cytotoxicity against cancer cells and was named WYC-241. Further investigation in A549 lung cancer cells showed that WYC-241 significantly inhibited co

SUBMITTER: Chu PY 

PROVIDER: S-EPMC12394904 | biostudies-literature | 2025 Aug

REPOSITORIES: biostudies-literature