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).

Graphical Abstract

Keywords:

• Oleanolic acid analogue
• structural modification
• molecular docking

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was financially supported by National Natural Science Foundation of China [21372156], the Liaoning Province key Research & Development project [2019JH2/10300034], the Department of Education Research Project of Liaoning Province [LFD2017004] and the Liaoning University Innovation Team Support Project of [LT2017009], the Key project of Shenyang University of Chemical Technology [LDB2019001].