Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor
文献类型：期刊论文
| 作者 | Wang, Xiaowen1,2; Su, Mingbo3,6; Li, You2,4; Liu, Tongchao2,5; Wang, Yujie3,6; Chen, Yabing2; Tang, Le2; He, Yu-Peng1; Ding, Xiaoguang1; Yu, Fang1 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2019-03-15 |
| 卷号 | 29期号:6页码:844-847 |
| 关键词 | LSD1 inhibitor Tranylcypromine Menin-MLL1 protei n-protein interaction inhibitor MV4-11 antiproliferative activity Structure activity relationship |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2019.01.017 |
| 通讯作者 | Yu, Fang(fang.yu@lnpu.edu.cn) ; Zhou, Yubo(ybzhou@simm.ac.cn) ; Chen, Yue-Lei(chenyuelei@gmail.com) ; Xiong, Bing(bxiong@simm.ac.cn) |
| 英文摘要 | Tranylcypromine moiety extracted from LSD1 inhibitors and 6-trifluoroethyl thienopyrimidine moiety from menin-MLL1 PPI inhibitors were merged to give new chemotypes for medicinal chemistry study. Among 15 new compounds prepared in this work, some exhibited nanomolar LSD1 activity and good selectivity over MAO-A/B, low micromolar menin-MLL1 PPI inhibitory activity, as well as submicromolar MV4-11 antiprofilative activities. Intracellular LSD1 engagement of compounds with higher enzymatic and antiproliferative activities was confirmed by CD86 mRNA up-regulation experiments. |
| WOS关键词 | DEMETHYLASE ; DESIGN ; POTENT |
| 资助项目 | National Natural Science Foundation of China[21877121] ; National Natural Science Foundation of China[81673309] ; National Natural Science Foundation of China[81330076] ; National Natural Science Foundation of China[81703544] ; National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China[2014ZX09507-002] ; Foundation of Liaoning Science and Technology Agency[20180550899] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000458623500016 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/290521]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Yu, Fang; Zhou, Yubo; Chen, Yue-Lei; Xiong, Bing |
| 作者单位 | 1.Liaoning Shihua Univ, Coll Chem Chem Engn & Environm Engn, Dandong Lu West 1, Fushun 113001, Peoples R China 2.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 3.Natl Ctr Drug Screening, 189 Guoshoujing Rd, Shanghai 201203, Peoples R China 4.China Pharmaceut Univ, Sch Pharm, 24 Tongjiaxiang, Nanjing 210009, Jiangsu, Peoples R China 5.Shenyang Pharmaceut Univ, Key Lab Struct Based Drug Design & Discovery, Minist Educ, 103 Wenhua Lu, Shenyang 110016, Liaoning, Peoples R China 6.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Xiaowen,Su, Mingbo,Li, You,et al. Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2019,29(6):844-847. |
| APA | Wang, Xiaowen.,Su, Mingbo.,Li, You.,Liu, Tongchao.,Wang, Yujie.,...&Xiong, Bing.(2019).Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,29(6),844-847. |
| MLA | Wang, Xiaowen,et al."Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 29.6(2019):844-847. |
入库方式： OAI收割
来源：上海药物研究所
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