| 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
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| 通讯作者 | yaoz@sioc.ac.cn ; qinshizhao@mail.kib.ac.cn |
| 2011-09-01 | |
| 发表期刊 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| ISSN | 0223-5234 |
| 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 |
| 学科领域 | Chemistry, Medicinal |
| DOI | 10.1016/j.ejmech.2011.06.028 |
| 收录类别 | SCI ; IC |
| 语种 | 英语 |
| WOS记录号 | WOS:000295237400074 |
| 引用统计 | |
| 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 |
| 推荐引用方式 GB/T 7714 | 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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