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2,4-Diarylamino-pyrimidines as kinase inhibitors co-targeting IGF1R and EGFR(L858R/T790M)

文献类型：期刊论文

作者Chan, Shingpan3,4; Han, Kun5; Qu, Rong4,5; Tong, Linjiang5; Li, Yingjun3,4; Zhang, Zhang1,3; Cheng, Huimin3; Lu, Xiaoyun3; Patterson, Adam2,6; Smaill, Jeff2,6
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2015-10-01
卷号25期号:19页码:4277-4281
关键词EGFR IGF1R NSCLC Dual inhibitor
ISSN号0960-894X
DOI10.1016/j.bmcl.2015.07.089
文献子类Article
英文摘要IGF1R amplification was recently implied to be related to the secondary acquired resistance against the 2nd or 3rd generation EGFR inhibitor therapies. We have successfully identified a series of 2,4-diarylamino-pyrimidines as new IGF1R/EGFR(L858R/T790M) co-targeting agents. One of the most promising compounds 8g potently inhibits both kinases with low nanomolar IC50 values, but is significantly less potent in inhibiting the wild type EGFR. The compound also displays a good kinase selectivity profile against a panel of 468 kinases. Moreover, 8g strongly suppresses the proliferation of CO-1686-resistant H1975-IGF1R cancer cells, suggesting its promising potential as a new lead compound for future anticancer drug discovery. (C) 2015 Elsevier Ltd. All rights reserved.
WOS关键词GROWTH-FACTOR RECEPTOR ; CELL LUNG-CANCER ; MULTITARGETED INHIBITORS ; EGFR ; RESISTANCE ; TRIAL ; CARBOPLATIN ; PACLITAXEL ; MUTATIONS ; GEFITINIB
资助项目Ministry of Science and Technology of China[2014DFG32100] ; National Natural Science Foundation of China[81425021] ; National Natural Science Foundation of China[81173080] ; National Natural Science Foundation of China[81321092] ; National High Technology Research and Development (863) for Young Scientists program of China[2015AA020906] ; Health Research Council of New Zealand[13/1020]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000361004700043
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/276391]  
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Xie, Hua
作者单位1.Jinan Univ, Guangzhou 510632, Guangdong, Peoples R China;
2.Univ Auckland, Maurice Wilkins Ctr Mol Biodiscovery, Auckland 1142, New Zealand
3.Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, State Key Lab Resp Dis, Guangzhou 510530, Guangdong, Peoples R China;
4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China;
5.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
6.Univ Auckland, Auckland Canc Soc Res Ctr, Auckland 1142, New Zealand;
推荐引用方式
GB/T 7714		 Chan, Shingpan,Han, Kun,Qu, Rong,et al. 2,4-Diarylamino-pyrimidines as kinase inhibitors co-targeting IGF1R and EGFR(L858R/T790M)[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2015,25(19):4277-4281.
APA Chan, Shingpan.,Han, Kun.,Qu, Rong.,Tong, Linjiang.,Li, Yingjun.,...&Ding, Ke.(2015).2,4-Diarylamino-pyrimidines as kinase inhibitors co-targeting IGF1R and EGFR(L858R/T790M).BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,25(19),4277-4281.
MLA Chan, Shingpan,et al."2,4-Diarylamino-pyrimidines as kinase inhibitors co-targeting IGF1R and EGFR(L858R/T790M)".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 25.19(2015):4277-4281.

入库方式： OAI收割

来源：上海药物研究所

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