Discovery and Structure-Activity Relationship Studies of Thiazole-Oxazole Tandem Heterocyclic RNA Splicing Inhibitors
文献类型：期刊论文
| 作者 | Zhang Rong3,4; Gao Xiang1,2,4; Chen Lingling1,2,4; Nan Fajun3,4
|
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2022-09-01 |
| 卷号 | 42期号:9页码:2925-2939 |
| 关键词 | splicing inhibitors circmCherry-expression system Leucamide A derivatives structure-activity relationships |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc202202033 |
| 通讯作者 | Nan Fajun(fjnan@simm.ac.cn) |
| 英文摘要 | Precursor mRNAs (pre-mRNAs) undergo splicing to remove introns and ligation of their exons to yield mature mRNAs. Pre-mRNA splicing is an essential component of gene expression and proteomic diversity in higher organisms. However, the alternative splicing or mutation of splicing factors have been found in human diseases. By the use of the small molecules modulate the splicing process will provide potential treatment for related diseases. In this paper, circmcherry expression system was used to screen compounds that could affect splicing process. Several simple derivatives of natural product Leucamide A have been found to have inhibitory effects, and 36 compounds with thiazole-oxazole tadem structural core were designed and synthesized, of which methyl 2-((S)-1-(2-(2-((S)-1-(4-methoxybenzamido)-2-methylpropyl)thiazol-4yl)-5-methyloxazole-4-carboxamido)ethyl)oxazole-4-carboxylate (9l) shows most potent inhibitory activity on splicing. |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000868890400025 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/303232]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Nan Fajun |
| 作者单位 | 1.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China 2.Shanghai Inst Biochem & Cell Biol, Shanghai 200031, Peoples R China 3.Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang Rong,Gao Xiang,Chen Lingling,et al. Discovery and Structure-Activity Relationship Studies of Thiazole-Oxazole Tandem Heterocyclic RNA Splicing Inhibitors[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2022,42(9):2925-2939. |
| APA | Zhang Rong,Gao Xiang,Chen Lingling,&Nan Fajun.(2022).Discovery and Structure-Activity Relationship Studies of Thiazole-Oxazole Tandem Heterocyclic RNA Splicing Inhibitors.CHINESE JOURNAL OF ORGANIC CHEMISTRY,42(9),2925-2939. |
| MLA | Zhang Rong,et al."Discovery and Structure-Activity Relationship Studies of Thiazole-Oxazole Tandem Heterocyclic RNA Splicing Inhibitors".CHINESE JOURNAL OF ORGANIC CHEMISTRY 42.9(2022):2925-2939. |
入库方式： OAI收割
来源：上海药物研究所
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