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| 柠檬烯类似物的合成及其体外抗癌活性 | |
| 引用本文： | 陈娇娇,刘冰弥,徐莉英,景永奎,董金华.柠檬烯类似物的合成及其体外抗癌活性[J].中国药物化学杂志,2006,16(6):356-359,379. |
| 作者姓名： | 陈娇娇 刘冰弥 徐莉英 景永奎 董金华 |
| 作者单位： | 1. 沈阳药科大学,制药工程学院,辽宁,沈阳,110016 2. 沈阳药科大学,制药工程学院,辽宁,沈阳,110016;辽宁大学,制药工程系,辽宁,沈阳,110036 3. Department of Medicine,Mount Sinai School of Medicine,New York,NY10029,USA |
| 摘 要： | 目的 设计并合成柠檬烯类似物,并对其体外抗癌活性进行初步的评价.方法 以l-香芹酮为起始原料,通过氯代、亲核取代、选择性还原制备目标化合物;以MTT法测试目标化合物对人前列腺癌细胞LNCaP的增殖抑制活性.结果与结论 所合成的14个新化合物经1H-NMR和MS确证结构.初步药理实验结果表明12个目标化合物的抗癌活性比d-柠檬烯和l-香芹酮更强. |
| 关 键 词： | 药物化学 化合物制备 柠檬烯衍生物 d-柠檬烯 l-香芹酮 抗肿瘤活性 |
| 文章编号： | 1005-0108（2006）06-0356-04 |
| 收稿时间： | 2006-06-12 |
| 修稿时间： | 2006-06-12 |
Synthesis of limonene derivatives and their antitumor activities in vitro |
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| CHEN Jiao-jiao,LIU Bing-mi,XU Li-ying,JING Yong-kui,DONG Jin-hua.Synthesis of limonene derivatives and their antitumor activities in vitro[J].Chinese Journal of Medicinal Chemistry,2006,16(6):356-359,379. | |
| Authors: | CHEN Jiao-jiao LIU Bing-mi XU Li-ying JING Yong-kui DONG Jin-hua |
| Institution: | 1. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China ; 2. Pharmaceutical Engineering Department, Liaoning University, Shen yang 110036, China ; 3. Department of Medicine, Mount Sinai School of Medicine, New York, NY10029, USA |
| Abstract: | Aim To design and synthesize limonene analogues, and to assess their antitumor activity in vitro. Methods The target compounds were synthesized from l-carvone via chlorination, nucleophilic substitution and selective reduction. Their in vitro antitumor activities were evaluated in prostate cell line LNCaP by using MTT assay. Results and conclusion The structures of 14 novel compounds were characterized by MS and ^1H-NMR. Preliminary pharmacological results showed that 12 compounds possessed stronger antitumor activities than d-limonene and l-carvone did in vitro. |
| Keywords: | medicinal chemistry compound preparation limonene derivatives d-lirnonene l -carvone antitumor activity |
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