Lathyrol Diterpenes as Modulators of P-Glycoprotein Dependent Multidrug Resistance: Structure-Activity Relationship Studies on Euphorbia Factor L-3 Derivatives
文献类型：期刊论文
| 作者 | Jiao, Wei; Wan, Zhongmin; Chen, Shuang; Lu, Runhua; Chen, Xiaozhen; Fang, Dongmei; Wang, Jiufeng; Pu, Shengcai; Huang, Xin; Gao, Haixiang |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2015 |
| 卷号 | 58期号:9页码:3720-3738 |
| 关键词 | MOUSE LYMPHOMA-CELLS JATROPHANE DITERPENES BREAST-CANCER MACROCYCLIC DITERPENES PROTEIN STRUCTURES DRUG-BINDING DISCOVERY TRANSPORTERS GENERATION DATABASE |
| 产权排序 | 1 |
| 通讯作者 | Jiao, W (reprint author), Chinese Acad Sci, Chengdu Inst Biol, Chengdu 610041, Peoples R China. |
| 合作状况 | 国内 |
| 英文摘要 | Five series of 37 new acylate and epoxide derivatives (3-39) of Euphorbia factor L3, a lathyrol diterpene isolated from Euphorbia lathyris, were designed by modifying the hydroxyl moiety of C-3, C-5, or C-15. Chemoreversal effects of the acylates on multidrug resistance (MDR) were evaluated in breast cancer multidrug-resistant MCF-7/ADR cells that overexpress P-glycoprotein (P-gp). Eight derivatives exhibited greater chemoreversal ability than verapamil (VRP) against adriamycin (ADR) resistance. Compounds 19 and 25 exhibited 4.8 and 4.0 times, respectively, more effective reversal ability than VRP against ADR resistance. To determine the key characteristics of Euphorbia factor L3 derivatives that contribute to MDR reversal, we conducted a structure-activity relationship study of these compounds. The simulation studies indicated different possible mechanisms and revealed the important influence of hydrophobic interactions and hydrogen bonds in the flexible cavity of P-gp. |
| 学科主题 | Pharmacology & Pharmacy |
| 类目[WOS] | Chemistry, Medicinal |
| 收录类别 | SCI |
| 语种 | 英语 |
| 源URL | [http://210.75.237.14/handle/351003/27584]  |
| 专题 | 成都生物研究所_天然产物研究 |
| 推荐引用方式 GB/T 7714 | Jiao, Wei,Wan, Zhongmin,Chen, Shuang,et al. Lathyrol Diterpenes as Modulators of P-Glycoprotein Dependent Multidrug Resistance: Structure-Activity Relationship Studies on Euphorbia Factor L-3 Derivatives[J]. JOURNAL OF MEDICINAL CHEMISTRY,2015,58(9):3720-3738. |
| APA | Jiao, Wei.,Wan, Zhongmin.,Chen, Shuang.,Lu, Runhua.,Chen, Xiaozhen.,...&Shao, Huawu.(2015).Lathyrol Diterpenes as Modulators of P-Glycoprotein Dependent Multidrug Resistance: Structure-Activity Relationship Studies on Euphorbia Factor L-3 Derivatives.JOURNAL OF MEDICINAL CHEMISTRY,58(9),3720-3738. |
| MLA | Jiao, Wei,et al."Lathyrol Diterpenes as Modulators of P-Glycoprotein Dependent Multidrug Resistance: Structure-Activity Relationship Studies on Euphorbia Factor L-3 Derivatives".JOURNAL OF MEDICINAL CHEMISTRY 58.9(2015):3720-3738. |
入库方式： OAI收割
来源：成都生物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。