Synthesis of gibberellin derivatives with anti-tumor bioactivities

  • Bioorg Med Chem Lett. 2009 Sep 15;19(18):5496-9. doi: 10.1016/j.bmcl.2009.07.090.
Jingbo Chen  1 ,  Zhuxian Sun ,  Yanli Zhang ,  Xianghui Zeng ,  Chen Qing ,  Jianping Liu ,  Liang Li ,  Hongbin Zhang
Affiliations
  • 1. Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming, Yunnan 650091, PR China.
PMID: 19679470 DOI: 10.1016/j.bmcl.2009.07.090
Abstract

A series of gibberellin based molecules were designed and synthesized. Gibberellin derivatives bearing two alpha,beta-unsaturated ketone units showed strong Anticancer activities in MTT assay towards a number of human Cancer cell lines including HT29, A549, HepG2 and MKN28. The most potent gibberellin derivative (compound 10, IC(50)=2.9 microM against HT29) inhibited completely the Topoisomerase I activity at 8 microg/mL level.