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 |
DOI | 10.1016/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
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。