Synthesis of oleanolic acid analogues targeting PDGF receptor inhibitors and their antitumor biological activities

Abstract

The PDGF receptor is mock-coupled with a known active compound, and 14 novel skeleton candidate compounds were designed and synthesized. The structure was confirmed by ¹H NMR, ¹³C NMR and MS. The in vitro cytotoxicity of the two cancer cell lines (SGC-7901 and A549) was evaluated by MTT assay. PDGF receptor protein inhibition assays were performed on I₆ and II₄ using fluorescence polarization immunoassay (FPIA). [Formula: see text].

Keywords: Oleanolic acid analogue; molecular docking; structural modification.