Synthesis and structure–activity relationship studies of MI-2 analogues as MALT1 inhibitors
文献类型：期刊论文
| 作者 | Ceshi Chen2; Rong Liu2; Jia Zhou4; Guolin Wu1; Haijun Chen1; Wenhui Zhou2,3; Wenhui Mo1; Bihua Zeng1; Kejie Zhu1 |
| 刊名 | Bioorganic & Medicinal Chemistry
 |
| 出版日期 | 2018 |
| 期号 | 26页码:3321–3344 |
| 关键词 | Malt1 Mi-2 Analogues Structure–activity Relationships Cancer Therapeutics |
| DOI | 10.1016/j.bmc.2018.04.059 |
| 英文摘要 | Recent studies revealed that MALT1 is a promising therapeutic target for the treatment of ABC-DLBCL.Among several reported MALT1 inhibitors, MI-2 as an irreversible inhibitor represents a new class ofABC-DLBCL therapeutics. Due to its inherent potential cross-reactivity, further structure–activity rela-tionship (SAR) study is imperative. In this work, five focused compound libraries based on the chemicalstructure of MI-2 are designed and synthesized. The systematic SARs revealed that the side chain of2-methoxyethoxy has little impact on the activity and can be replaced by other functionalized groups,providing new MI-2 analogues with retained or enhanced potency. Compounds 81–83 with terminalhydroxyl group as side chain displayed enhanced activities against MALT1. Replacement of triazole corewith pyrazole is also tolerant, while structural modifications on other sites are detrimental. Thesefindings will facilitate further development of small-molecule MALT1 inhibitors. |
| 语种 | 英语 |
| 源URL | [http://159.226.149.26:8080/handle/152453/12355]  |
| 专题 | 昆明动物研究所_肿瘤生物学 |
| 通讯作者 | Ceshi Chen |
| 作者单位 | 1.College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, China 2.Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology Kunming, Yunnan 650223, China 3.Hubei Key Laboratory of Embryonic Stem Cell Research, Biomedical Research Institute, Hubei University of Medicine, Shiyan, Hubei 442000, China 4.Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, USA 5.University of Science and Technology of China, Hefei, Anhui 230027, China |
| 推荐引用方式 GB/T 7714 | Ceshi Chen,Rong Liu,Jia Zhou,et al. Synthesis and structure–activity relationship studies of MI-2 analogues as MALT1 inhibitors[J]. Bioorganic & Medicinal Chemistry,2018(26):3321–3344. |
| APA | Ceshi Chen.,Rong Liu.,Jia Zhou.,Guolin Wu.,Haijun Chen.,...&Kejie Zhu.(2018).Synthesis and structure–activity relationship studies of MI-2 analogues as MALT1 inhibitors.Bioorganic & Medicinal Chemistry(26),3321–3344. |
| MLA | Ceshi Chen,et al."Synthesis and structure–activity relationship studies of MI-2 analogues as MALT1 inhibitors".Bioorganic & Medicinal Chemistry .26(2018):3321–3344. |
入库方式： OAI收割
来源：昆明动物研究所
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。