Syntheses and structure-activity relationship studies of N-substituted-β-D-glucosaminides as selective cytotoxic agents

  • Bioorg Med Chem Lett. 2012 Dec 1;22(23):7110-3. doi: 10.1016/j.bmcl.2012.09.075.
Bo Wang  1 ,  Yang Liu ,  Yanshi Wang ,  Xin Liu ,  Mao-Sheng Cheng
Affiliations
  • 1. Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
PMID: 23067549 DOI: 10.1016/j.bmcl.2012.09.075
Abstract

Twenty-four diosgenyl saponins bearing cinnamoyl, carbamido and thiosemicarbazone groups were synthesized concisely. The cytotoxicities of the synthetic compounds on six human caner cell lines were evaluated employing MTT method. Structure-activity relationship could be observed, and two of the synthesized compounds (5c and 5f) exhibited selective inhibition on HeLa and MCF-7 cells, while three of them (5d, 5f and 5h) showed strong inhibition against HT1080.