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论文 |
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论文题目: |
Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles
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论文题目英文: |
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作者: |
Deng, Xu; Su, Jia; Zhao, Yu; Peng, Li-Yan; Li, Yan; Yao, Zhu-Jun; Zhao, Qin-Shi
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论文出处: |
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年: |
2011
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卷: |
46 |
期: |
9 |
页: |
4238-4244 |
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发表期刊: |
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY |
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影响因子: |
2.882
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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. |
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