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: slcui@zju.edu.cn.
3 Institute of Materia Medica and College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China. Electronic address: tingjunhou@zju.edu.cn.

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.

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