An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core
文献类型：期刊论文
| 作者 | Song, Zilan3; Xia, Zongjun1,2,4; Ji, Yinchun1; Xing, Li3; Gao, Yinglei1; Ai, Jing1 ; Geng, Meiyu1,4; Zhang, Ao2,3
|
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2016-08-08 |
| 卷号 | 118页码:244-249 |
| 关键词 | Benzo[b]carbazolones ALK inhibitors RET kinase Antiresistance Non-small-cell lung cancer Preclinical study |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2016.04.046 |
| 文献子类 | Article |
| 英文摘要 | Our early structure-activity relationship study has identified benzo[b]carbazolone 6 as a high potency orally bioavailable ALK inhibitor. Further lead profiling disclosed that 6 is active against both ALK resistant and hot spot-activating mutants, and is also highly potent against RET kinase. Tumor stasis and partial tumor regression were achieved with 6 in both NIH/3T3-EML4-ALK and NIH/3T3-EML4-ALK L1196M xenograft models. Based on the optimal in vitro and in vivo antitumor efficacy, compound 6 is now being profiled further in our preclinical settings as a new orally available ALK/RET dual inhibitor. (C) 2016 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | ANAPLASTIC LYMPHOMA KINASE ; CELL LUNG-CANCER ; POTENT ; DESIGN ; CHALLENGES ; RESISTANCE ; ALECTINIB |
| 资助项目 | Chinese NSF[81430080] ; Chinese NSF[81373277] ; Chinese NSF[81473243] ; Chinese NSF[81321092] ; National Science & Technology Major Project on 'Key New Drug Creation and Manufacturing Program', China[2012ZX09103-101-035] ; National Science & Technology Major Project on 'Key New Drug Creation and Manufacturing Program', China[2012ZX09301001-007] ; SIMM[CASIMM0120154002/2002] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000377312400021 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275930]  |
| 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 药物化学研究室 |
| 通讯作者 | Ai, Jing; Geng, Meiyu; Zhang, Ao |
| 作者单位 | 1.Chinese Acad Sci, SIMM, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China; 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Chinese Acad Sci, SIMM, CAS Key Lab Receptor Res, Synthet Organ & Med Chem Lab, Shanghai 201203, Peoples R China; 4.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 200031, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Song, Zilan,Xia, Zongjun,Ji, Yinchun,et al. An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2016,118:244-249. |
| APA | Song, Zilan.,Xia, Zongjun.,Ji, Yinchun.,Xing, Li.,Gao, Yinglei.,...&Zhang, Ao.(2016).An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,118,244-249. |
| MLA | Song, Zilan,et al."An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 118(2016):244-249. |
入库方式： OAI收割
来源：上海药物研究所
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。