Synthesis and structure-activity relationship studies of LLY-507 analogues as SMYD2 inhibitors
文献类型：期刊论文
| 作者 | Zhang, Bin2; Liao, Liping1,3; Wu, Fan2; Zhang, Fengcai1,3; Sun, Zhongya1,3; Chen, Haijun2; Luo, Cheng1,3
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2020-11-15 |
| 卷号 | 30期号:22页码:5 |
| 关键词 | SMYD2 inhibitors Thermal shift assay Structure-activity relationships |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2020.127598 |
| 通讯作者 | Chen, Haijun(chenhaij@gmail.com) |
| 英文摘要 | SET and MYND domain-containing protein 2 (SMYD2), a lysine methyltransferase, is reported to catalyze the methylation of lysine residues on histone and non-histone proteins. As a potential target for cancer therapy, there are several SMYD2 inhibitors are reported, LLY-507 as a cell-active inhibitor exhibits submicromolar potency against SMYD2 in several cancer cell lines. To know which structural fragment of LLY-507 is suitable for chemical modification, three sites are chosen for structure-activity relationship studies (SARs). Among our focused library, compounds 43 and 44 with amide link on site C showed reasonably improved potency indicating that modification on this fragment is more flexible and introduction of electrophilic warheads in this position might provide lysine-targeting covalent inhibitors for SMYD2. |
| WOS关键词 | METHYLTRANSFERASE SMYD2 ; LYSINE ; DISCOVERY ; METHYLATION ; INSIGHTS ; FAMILY |
| 资助项目 | Natural Science Foundation of Fujian Province[2019J01202] ; Natural Science Foundation of China[81625022] ; Natural Science Foundation of China[91853205] ; Natural Science Foundation of China[81821005] ; K. C. Wong Education Foundation |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000594726800001 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/296254]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Chen, Haijun |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 2.Fuzhou Univ, Key Lab Mol Synth & Funct Discovery, Coll Chem, Fujian Prov Univ, Fuzhou 350116, Fujian, Peoples R China 3.Univ Chinese Acad Sci, 19 Yuquan Rd, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Bin,Liao, Liping,Wu, Fan,et al. Synthesis and structure-activity relationship studies of LLY-507 analogues as SMYD2 inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2020,30(22):5. |
| APA | Zhang, Bin.,Liao, Liping.,Wu, Fan.,Zhang, Fengcai.,Sun, Zhongya.,...&Luo, Cheng.(2020).Synthesis and structure-activity relationship studies of LLY-507 analogues as SMYD2 inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,30(22),5. |
| MLA | Zhang, Bin,et al."Synthesis and structure-activity relationship studies of LLY-507 analogues as SMYD2 inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 30.22(2020):5. |
入库方式： OAI收割
来源：上海药物研究所
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