Synthesis of gibberellin derivatives with anti-tumor bioactivities.

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.

• Authors: Jingbo Chen, Zhuxian Sun, Yanli Zhang, Xianghui Zeng, Chen Qing, Jianping Liu, Liang Li, Hongbin Zhang
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 19 Issue 18 Pg. 5496-9 (Sep 15 2009) ISSN: 1464-3405 [Electronic] England
• PMID: 19679470 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Gibberellins
• Topoisomerase I Inhibitors
• DNA Topoisomerases, Type I

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Cell Survival (drug effects)
• DNA Topoisomerases, Type I (metabolism)
• Drug Screening Assays, Antitumor
• Gibberellins (chemical synthesis, chemistry, pharmacology)
• Humans
• Inhibitory Concentration 50
• Neoplasms (drug therapy)
• Structure-Activity Relationship
• Topoisomerase I Inhibitors