Jatrophanes as promising multidrug resistance modulators: Advances of structure-activity relationships
文献类型：期刊论文
| 作者 | Li, Jun1,2 ; Wang, Wen-qiong1,2; Tang, Shuai1,2; Song, Wei-bin1,2; Xuan, Li-jiang1,2
|
| 刊名 | FITOTERAPIA
 |
| 出版日期 | 2018-06 |
| 卷号 | 127页码:138-145 |
| 关键词 | Euphorbia helioscopia Multidrug resistance Jatrophanes |
| ISSN号 | 0367-326X |
| DOI | 10.1016/j.fitote.2018.02.014 |
| 文献子类 | Article |
| 英文摘要 | The phytochemical study of Euphorbia helioscopia afforded euphornin (1) in a large amount. Alkaline hydrolysis of 1 using potassium carbonate yielded the main product monodeacetyleuphornin (2), whose structural modification at 14-OH gave rise to 21 acylated derivatives euphornoate A-U (3-23). Thus, a mini compound library of jatrophanes was established to screen for MDR modulators. Biological studies clearly demonstrated the effect of C-14 pattern modification in MDR reversal activity and several compounds with RF values over 300 fold at 20 mu m (6, 16, 20, 22, 23) were thought to be promising MDR modulators. The SARs are discussed, which reveal that introduction of an alkyl acyl group bearing 4 carbons at C-14 or an aryl acyl group with electron donating groups is favorable for the activity. |
| WOS关键词 | HUMAN COLON ADENOCARCINOMA ; EUPHORBIA-HELIOSCOPIA ; DRUG TRANSPORTERS ; DITERPENES ; DISCOVERY ; CANCER ; AGENTS ; CHEMOTHERAPY ; DERIVATIVES ; LYMPHOMA |
| 资助项目 | State Key Laboratory of Drug Research[SIMM1601ZZ-03] ; China Postdoctoral Science Foundation[2016M600345] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000437551000021 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279717]  |
| 专题 | 上海中药现代化研究中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 所领导 |
| 通讯作者 | Xuan, Li-jiang |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Meteria Med, State Key Lab Drug Res, 501 Haike Rd, Shanghai 201201, Peoples R China; 2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Jun,Wang, Wen-qiong,Tang, Shuai,et al. Jatrophanes as promising multidrug resistance modulators: Advances of structure-activity relationships[J]. FITOTERAPIA,2018,127:138-145. |
| APA | Li, Jun,Wang, Wen-qiong,Tang, Shuai,Song, Wei-bin,&Xuan, Li-jiang.(2018).Jatrophanes as promising multidrug resistance modulators: Advances of structure-activity relationships.FITOTERAPIA,127,138-145. |
| MLA | Li, Jun,et al."Jatrophanes as promising multidrug resistance modulators: Advances of structure-activity relationships".FITOTERAPIA 127(2018):138-145. |
入库方式： OAI收割
来源：上海药物研究所
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