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

Xiao-Juan Wang; Hai-Wei Xu; Lin-Lin Guo; Jia-Xin Zheng; Bo Xu; Xiao Guo; Chen-Xin Zheng; Hong-Min Liu

doi:10.1016/j.bmcl.2011.03.029

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. Epub 2011 Mar 17.

Authors

Xiao-Juan Wang¹, Hai-Wei Xu, Lin-Lin Guo, Jia-Xin Zheng, Bo Xu, Xiao Guo, Chen-Xin Zheng, Hong-Min Liu

Affiliation

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

4-Butyrolactone / analogs & derivatives*
4-Butyrolactone / chemistry
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Cell Proliferation / drug effects
Drug Design*
Humans
Inhibitory Concentration 50
Magnetic Resonance Spectroscopy
Molecular Structure
Structure-Activity Relationship
Thiocarbamates / chemical synthesis*
Thiocarbamates / chemistry
Thiocarbamates / pharmacology*

Substances

Antineoplastic Agents
Thiocarbamates
butenolide
4-Butyrolactone