中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo [2,1-f] [1,2,4] triazine derivatives

文献类型:期刊论文

作者Xiang, Hao-Yue1,2; Chen, Yan-Hong2; Wang, Yi2; Zhang, Xi2; Ding, Jian2; Meng, Ling-Hua2; Yang, Chun-Hao2
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2020-06-15
卷号30期号:12页码:4
ISSN号0960-894X
关键词Antiproliferative Cancer Therapy PI3K inhibitors Pyrrolo [2,1-f][1,2,4] triazine Kinase
DOI10.1016/j.bmcl.2020.127194
通讯作者Meng, Ling-Hua(lhmeng@simm.ac.cn) ; Yang, Chun-Hao(chyang@simm.ac.cn)
英文摘要A series of 6-aminocarbonyl pyrrolo [2,1-f] [1,2,4]triazine derivatives were designed by scaffold hopping strategy. The IC50 values of compound 14a against PI3Ks were measured, showing selective activity against p110 alpha and p110 delta with IC(50)s of 122 nM and 119 nM respectively. All the synthesized compounds were evaluated for their antiproliferative activity against human cancer cells by SRB assay. Compounds 14a, 14p and 14q exhibited potent antiproliferative activity against five types of human cancer cells and the PK property of 14q was also investigated here.
WOS关键词SMALL-MOLECULE INHIBITORS ; I PI3 KINASE ; 3-KINASE ; IDENTIFICATION ; POTENT ; DISCOVERY ; PATHWAY
资助项目National Natural Science Foundation of China[90713034] ; National Natural Science Foundation of China[81703365] ; Institutes for Drug Discovery and Development, Chinese Academy of Sciences[CASIMM0120185009] ; State Key Laboratory of Drug Research Program[SIMM1705KF-15]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
出版者PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号WOS:000536454600007
源URL[http://119.78.100.183/handle/2S10ELR8/280036]  
专题新药研究国家重点实验室
通讯作者Meng, Ling-Hua; Yang, Chun-Hao
作者单位1.Cent South Univ, Coll Chem & Chem Engn, Changsha 410083, Hunan, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714
Xiang, Hao-Yue,Chen, Yan-Hong,Wang, Yi,et al. Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo [2,1-f] [1,2,4] triazine derivatives[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2020,30(12):4.
APA Xiang, Hao-Yue.,Chen, Yan-Hong.,Wang, Yi.,Zhang, Xi.,Ding, Jian.,...&Yang, Chun-Hao.(2020).Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo [2,1-f] [1,2,4] triazine derivatives.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,30(12),4.
MLA Xiang, Hao-Yue,et al."Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo [2,1-f] [1,2,4] triazine derivatives".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 30.12(2020):4.

入库方式: OAI收割

来源:上海药物研究所

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