Synthesis and cytotoxicity of 2-cyano-28-hydroxy-lup-1-en-3-ones

  • Bioorg Med Chem Lett. 2009 Apr 15;19(8):2168-71. doi: 10.1016/j.bmcl.2009.02.107.
Ali Koohang  1 ,  Nathan D Majewski ,  Erika L Szotek ,  Aye Aye Mar ,  David A Eiznhamer ,  Michael T Flavin ,  Ze-Qi Xu
Affiliations
  • 1. Advanced Life Sciences, Inc, Research and Development, Woodridge, IL 60517, USA.
PMID: 19286375 DOI: 10.1016/j.bmcl.2009.02.107
Abstract

New A-ring modified betulin and dihydrobetulin derivatives possessing the 2-cyano-1-en-3-one moiety were prepared and tested for cytotoxicity in seven Cancer cell lines. The most active agent 9a synthesized in this account was further demonstrated to induce Apoptosis and to activate caspases in malignant melanoma cells.