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Bioorganic and Medicinal Chemistry Letters 2009-Sep

Synthesis of gibberellin derivatives with anti-tumor bioactivities.

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Jingbo Chen
Zhuxian Sun
Yanli Zhang
Xianghui Zeng
Chen Qing
Jianping Liu
Liang Li
Hongbin Zhang

Keywords

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.

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