oblongifolin-c and benzophenone

Oblongifolin C, one of the polyprenylated benzoylphloroglucinol natural products (PPAPs) isolated from the fruits of Garcinia yunnanensis Hu, was recently discovered to be a potent anti-tumor agent. A collection of 12 derivatives with modifications on the benzophenone moieties were synthesized and tested for c-Met kinase inhibition and cytotoxicity against the HepG2, Miapaca-2, HCC827, Hela, A549, AGS, and HT-29 cell lines in vitro. An oxidized derivative, 10, was found to possess strong inhibition and anti-migration properties in the HCC827 cell line and serves as a potential lead compound for the development of new anticancer drugs. In addition, structure-activity relationships (SAR) were also evaluated to provide key information for future anticancer drug development.

Topics: Antineoplastic Agents, Phytogenic; Benzophenones; Cell Line, Tumor; Drug Screening Assays, Antitumor; Garcinia; HeLa Cells; HT29 Cells; Humans; Neoplasms; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-met; Structure-Activity Relationship; Terpenes