Synthesis and in vitro cytotoxic activity evaluation of novel heterocycle bridged carbothioamide type isosteviol derivatives as antitumor agents

  • Bioorg Med Chem Lett. 2013 Mar 1;23(5):1343-6. doi: 10.1016/j.bmcl.2012.12.091.
Song-Lin Zhu  1 ,  Ya Wu ,  Cong-Jun Liu ,  Chang-Yong Wei ,  Jing-Chao Tao ,  Hong-Min Liu
Affiliations
  • 1. New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100 KeXue Avenue, Zhengzhou, Henan 450001, China.
PMID: 23347685 DOI: 10.1016/j.bmcl.2012.12.091
Abstract

Two series of novel carbothioamide-substituted pyrazole and isoxazolidine derivatives were facilely prepared by functional interconversions in ring D of the tetracyclic diterpene isosteviol. The in vitro cytotoxic activities against four human tumor cell lines were evaluated. Our results indicated that carbothioamide-substituted pyrazole derivatives exhibited noteworthy cytotoxic activities. Specifically, compound 12p (IC(50)=6.51 μM) had the most potent cytotoxicity against Raji cell, which may be exploitable as a lead compound for the development of potent antitumor agents.