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题名: Dual-Functional abeo-Taxane Derivatives Destabilizing Microtubule Equilibrium and Inhibiting NF-kappa B Activation
作者: Zhao, Yu1, 2; Su, Jia1, 3; Goto, Masuo2; Morris-Natschke, Susan L.2; null(李艳)1; null(赵勤实)1; Yao, Zhu-Jun4; Lee, Kuo-Hsiung2, 5, 6
刊名: JOURNAL OF MEDICINAL CHEMISTRY
关键词: NATURAL-PRODUCTS ; BIOLOGICAL-ACTIVITY ; CANCER-THERAPY ; PACLITAXEL ; TAXOL ; RESISTANCE ; DRUGS ; CHEMOTHERAPY ; PARTHENOLIDE ; BREVIFOLIOL
英文摘要: Taxchinin A, with a 11(15 -> 1)-abeo-taxane skeleton, is a major, but inactive taxoid contained in leaves of Taxus chinensis. In our design of dual-functional antitumor abeo-taxane derivatives, two fragments from antitumor agents with different molecular targets (the N-acyl-3'-phenylisoserine side chain from the antimitotic agent paclitaxel and an alpha,beta-unsaturated carbonyl system from NF-kappa B inhibitors) were incorporated into the scaffold of taxchinin A. The resulting compounds displayed broad inhibitory effects against proliferation of tumor cell lines, with notable selectivity toward colon cancer, melanoma, and renal cancer, when evaluated in the NCI-60 human tumor cell line screening panel. On the basis of the NCI-60 assay data, structure-activity relationship (SAR) correlations were elucidated. Mechanistic studies indicated that this new compound type can both destabilize microtubules and inhibit NF-kappa B activation, thereby inducing tumor cell apoptosis. This first report of the dual-functional taxoid-core compounds thus provides new opportunities for future drug development based on natural axoid scaffolds.
出版日期: 2013-06-13
卷号: 56, 期号:11, 页码:4749-4757
语种: 英语
收录类别: SCI ; IC
学科分类: Chemistry, Medicinal
ISSN号: 0022-2623
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/16763
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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作者单位: 1.Chinese Acad Sci, State Key Lab Phytochem & Plant Resources West Ch, Kunming Inst Bot, Kunming 650204, Peoples R China
2.Univ N Carolina, Nat Prod Res Labs, UNC Eshelman Sch Pharm, Chapel Hill, NC 27599 USA
3.Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Organ Chem, State Key Lab Bioorgan & Nat Prod Chem, EISU Chem Biol Div, Shanghai 200032, Peoples R China
5.Univ N Carolina, UNC Lineberger Comprehens Canc Ctr, Chapel Hill, NC 27599 USA
6.China Med Univ & Hosp, Chinese Med Res & Dev Ctr, Taichung 40447, Taiwan

Recommended Citation:
Zhao, Yu; Su, Jia; Goto, Masuo; Morris-Natschke, Susan L.; Li, Yan; Zhao, Qin-Shi; Yao, Zhu-Jun; Lee, Kuo-Hsiung.Dual-Functional abeo-Taxane Derivatives Destabilizing Microtubule Equilibrium and Inhibiting NF-kappa B Activation,JOURNAL OF MEDICINAL CHEMISTRY,2013,56(11):4749-4757
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