Synthesis and antiproliferative evaluation of 2-hydroxylated (E)-stilbenes

  • Bioorg Med Chem Lett. 2014 Dec 1;24(23):5470-2. doi: 10.1016/j.bmcl.2014.10.009.
Yan Zhang  1 ,  Mingyun Shen  1 ,  Sunliang Cui  2 ,  Tingjun Hou  3
Affiliations
  • 1. Institute of Materia Medica and College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
  • 2. Institute of Materia Medica and College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China. Electronic address: [email protected].
  • 3. Institute of Materia Medica and College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China. Electronic address: [email protected].
PMID: 25455486 DOI: 10.1016/j.bmcl.2014.10.009
Abstract

A simple synthesis of 2-hydroxylated (E)-stilbenes was accomplished in good yields via oxidative coupling of 2-hydroxystyrenes and arylboronic acids, with Rh(III)-catalyst and Cu(OAc)2 as oxidant. The antiproliferative evaluation of all the synthesized compounds were assessed on four different human Cancer cell lines (Colo-205, MDA-468, HT29, and MGC80-3), and the results showed that several compounds exhibit strong antiproliferative activities (up to IC50=35 nM for MGC80-3).

Keywords
2-Hydroxylated (E)-stilbenes; 2-Hydroxystyrenes; Antiproliferative; Arylboronic acids; Oxidative coupling.