2. Academic Validation
  3. Synthesis and antitumor activity of feruloyl and caffeoyl derivatives

Synthesis and antitumor activity of feruloyl and caffeoyl derivatives

  • Bioorg Med Chem Lett. 2014 Sep 15;24(18):4367-4371. doi: 10.1016/j.bmcl.2014.08.024.
Hui-Zhen Chen 1,  You-Bao Chen 2,  Ya-Ping Lv 2,  Fang Zeng 2,  Juan Zhang 2,  Yong-Lie Zhou 3,  Han-Bing Li 2,  Li-Fei Chen 4,  Bin-Jie Zhou 5,  Jian-Rong Gao 2,  Chun-Nian Xia 6
Affiliations

Affiliations

  • 1 Sir Run Run Shaw Hospital, Zhejiang University, Hangzhou 310016, People's Republic of China.
  • 2 College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China.
  • 3 Zhejiang Province People's Hospital, Hangzhou 310014, People's Republic of China.
  • 4 Zhejiang Hisun Pharmaceutical Co. Ltd., 46 Waisha Road, Jiaojiang District, Taizhou City, Zhejiang Province 318000, People's Republic of China.
  • 5 Ningbo Green-Health Pharmaceutical Co., Ltd, Fenghua Xiwu Town Foreign Technological Garden, Ningbo 315505, People's Republic of China.
  • 6 College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China. Electronic address: xcn77@zjut.edu.cn.
PMID: 25160837 DOI: 10.1016/j.bmcl.2014.08.024
Abstract

We developed two efficient protocols for the synthesis of feruloyl and caffeoyl derivatives from commercial vanillin and veratraldehyde. Pharmacological activities were assessed against a panel of human Cancer cell lines in vitro. Most synthesized compounds demonstrated attractive cytotoxicity. Several new compounds demonstrated significant antiproliferative and cytotoxic activities against HeLa and Bewo tumor cell lines. In particular, 5-nitro caffeic adamantyl ester showed broad spectrum of tumor inhibition in 10 cell lines, and reduced tumor weight by 36.7% in vivo when administered at a dose of 40 mg kg(-1).

Keywords

Antitumor; Caffeoyl; Feruloyl; SARs.

Figures