Synthesis and biological evaluation of novel larotaxel analogues
文献类型：期刊论文
| 作者 | Ren, Sumei2; Wang, Yujie2; Wang, Junfei2; Gao, Dingding2; Zhang, Minmin1 ; Ding, Ning2,4; Li, Yingxia2,3
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2018-08-05 |
| 卷号 | 156页码:692-710 |
| 关键词 | Larotaxel Toxoids Structure-activity relationship Semi-synthesis Drug-resistant Cytotoxicity |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2018.07.029 |
| 文献子类 | Article |
| 英文摘要 | Taxoids are a class of successful drugs and have been successfully used in chemotherapy for a variety of cancer types. However, despite the hope and promises that these taxoids have engendered, their utility is hampered by some clinic limitations. Extensive structure-activity relationship (SAR) studies of toxoids have been performed in many different laboratories. Whereas, SAR studies that based on the new generation toxoid, larotaxel, have not been reported yet. In view of the advantages in preclinical and clinical data of larotaxel over former toxoids, new taxoids that strategicly modified at the C3'/C3'-N and C2 positions of larotaxel were designed, semi-synthesized, and examined for their potency and efficacy in vitro. As a result, it has been shown that the majority of these larotaxel analogues are exceptionally potent against both drug-sensitive tumor cells and tumor cells with drug resistance arising from P-glycoprotein over expression. Further in vivo antitumor efficacies investigations revealed A2 might be a potent antitumor drug candidate for further preclinical evaluation. (C) 2018 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | NEW-GENERATION TAXOIDS ; RACEMIC BETA-LACTAMS ; 2ND-GENERATION TAXOIDS ; KINETIC RESOLUTION ; PACLITAXEL ; DOCETAXEL ; BINDING ; CONFORMATION ; CHEMISTRY ; TAXANES |
| 资助项目 | National Major Scientific and Technological Special Project of China for "Significant New Drugs Development"[2018ZX09711002-003-009] ; National Major Scientific and Technological Special Project of China for "Significant New Drugs Development"[2018ZX09711002-006-008] ; Shanghai Science and Technology Innovation Fund[17431902400] ; Shanghai Talent Development Fund (2017)[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000443663200051 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279625]  |
| 专题 | 药理学第一研究室 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 |
| 通讯作者 | Ding, Ning; Li, Yingxia |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Fudan Univ, Sch Pharm, Dept Med Chem, Shanghai 201203, Peoples R China; 3.Pilot Natl Lab Marine Sci & Technol, Lab Marine Drugs & Biol Prod, Qingdao 266237, Peoples R China; 4.Fudan Univ, Zhangjiang Technol Inst, 825 Zhangheng Rd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ren, Sumei,Wang, Yujie,Wang, Junfei,et al. Synthesis and biological evaluation of novel larotaxel analogues[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2018,156:692-710. |
| APA | Ren, Sumei.,Wang, Yujie.,Wang, Junfei.,Gao, Dingding.,Zhang, Minmin.,...&Li, Yingxia.(2018).Synthesis and biological evaluation of novel larotaxel analogues.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,156,692-710. |
| MLA | Ren, Sumei,et al."Synthesis and biological evaluation of novel larotaxel analogues".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 156(2018):692-710. |
入库方式： OAI收割
来源：上海药物研究所
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