Synthesis and in vitro antitumor activity of new butenolide-containing dithiocarbamates

  • Bioorg Med Chem Lett. 2011 May 15;21(10):3074-7. doi: 10.1016/j.bmcl.2011.03.029.
Xiao-Juan Wang  1 ,  Hai-Wei Xu ,  Lin-Lin Guo ,  Jia-Xin Zheng ,  Bo Xu ,  Xiao Guo ,  Chen-Xin Zheng ,  Hong-Min Liu
Affiliations
  • 1. New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, PR China.
PMID: 21486694 DOI: 10.1016/j.bmcl.2011.03.029
Abstract

Three series of butenolide-containing dithiocarbamates were designed and synthesized. Their anti-tumor activity in vitro was evaluated. Among them compound I-14 exhibited broad spectrum anti-cancer activity against five human Cancer cell lines with IC(50) <30 μM. Structure-activity relationship analysis showed that the introduction of dithiocarbamate side chains on the C-3 position of butenolide was crucial for anti-tumor activity.