Synthesis of gibberellin derivatives with anti-tumor bioactivities.
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.
Chen
Jingbo
J
Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming, Yunnan 650091, PR China.
Sun
Zhuxian
Z
Zhang
Yanli
Y
Zeng
Xianghui
X
Qing
Chen
C
Liu
Jianping
J
Li
Liang
L
Zhang
Hongbin
H
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004264:DNA Topoisomerases, Type I / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D005875:Gibberellins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D009369:Neoplasms / Q000188:drug therapy; D013329:Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors
D000970:Antineoplastic Agents; D005875:Gibberellins; D059004:Topoisomerase I Inhibitors; D004264:DNA Topoisomerases, Type I