Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles
Deng, Xu1,3; Su, Jia1; Zhao, Yu1; Peng, Li-Yan1; Li, Yan1; Yao, Zhu-Jun2; Zhao, Qin-Shi1
2011-09-01
发表期刊EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
卷号46期号:9页码:4238-4244
摘要Cheliensisin A is a natural styryl-lactone isolated from Goniothalamus cheliensis Hu in considerably large quantity with putative anticancer activities. However, its poor water solubility and chemical instability have precluded cheliensisin A as a potential drug candidate. To explore the strategy to overcome these problems, 21 novel derivatives of cheliensisin A with different substitutions at C-7 and C-8 positions were designed and synthesized. Inhibition of proliferation against five tumors cell lines indicates that eight new derivatives with embedment of oxazole or oxazoline exhibit improved cytotoxicity on SK-BR-3 and PANC-1, and compounds 2d and 2g show 5-8 folds higher potency than cisplatin. HPLC investigation of representative compounds indicates that oxazole and oxazoline analogs exhibit much improved chemical stability than their natural parent. (C) 2011 Elsevier Masson SAS. All rights reserved.
关键词Cheliensisin a Derivative Structure-activity Relationship Cytotoxicity Anticancer
资助信息National Natural Science Foundation of China[90813004, 20802083, U0932602]; State Key Laboratory of Phytochemistry and Plant Resources in West China[P2010-ZZ18]
学科领域Chemistry, Medicinal
DOI10.1016/j.ejmech.2011.06.028
收录类别SCI ; IC
语种英语
WOS研究方向Pharmacology & Pharmacy
WOS类目Chemistry, Medicinal
WOS记录号WOS:000295237400074
引用统计
被引频次:7[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/3938
专题中国科学院东亚植物多样性与生物地理学重点实验室
作者单位1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Organ Chem, State Key Lab Bioorgan & Nat Prod Chem, Shanghai 200032, Peoples R China
3.Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China
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Deng, Xu,Su, Jia,Zhao, Yu,et al. Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2011,46(9):4238-4244.
APA Deng, Xu.,Su, Jia.,Zhao, Yu.,Peng, Li-Yan.,Li, Yan.,...&Zhao, Qin-Shi.(2011).Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,46(9),4238-4244.
MLA Deng, Xu,et al."Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 46.9(2011):4238-4244.
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