An efficient and concise synthesis of a selective small molecule non-peptide inhibitor of cathepsin L: KGP94
文献类型：期刊论文
| 作者 | Munikishore,Rachakunta; Wang,Liang-Liang; Zhang,Shuqun; Zhao,Qin-Shi; Zuo,Zhili
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| 刊名 | BIOORGANIC CHEMISTRY
 |
| 出版日期 | 2021 |
| 卷号 | 116页码:105317 |
| 关键词 | Cathepsin L small-molecule inhibitor gram-scale synthesis KGP94 cancer FUNCTIONALIZED BENZOPHENONE BIOLOGICAL EVALUATION TUMOR PROGRESSION CELL INVASION EXPRESSION ANALOGS SUPPRESSION DERIVATIVES ACID |
| ISSN号 | 0045-2068 |
| DOI | 10.1016/j.bioorg.2021.105317 |
| 英文摘要 | KGP94 is a potent, selective, and competitive inhibitor of the lysosomal endopeptidase enzyme (Cathepsin L) currently in preclinical trials for the treatment of metastatic cancer, which is a leading cause of cancer-associated death. Herein, we report two new synthetic routes for synthesizing the target compound through four consecutive steps, using a Weinreb amide approach starting from a common 3-bromobenzoyl chloride. A key step in the approach is a coupling reaction of a readily available Grignard reagent with amide 4 to produce 6, a previously unreported coupling pattern. These new strategies offer an efficient and alternative approach to synthesis of target compound with an excellent overall yield. |
| WOS记录号 | WOS:000701702300006 |
| 源URL | [http://ir.kib.ac.cn/handle/151853/73249]  |
| 专题 | 中国科学院昆明植物研究所 |
| 作者单位 | 1.Zhao, Qin-Shi 2.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China 3.Wang, Liang-Liang 4.Zhang, Shuqun 5.[Munikishore, Rachakunta |
| 推荐引用方式 GB/T 7714 | Munikishore,Rachakunta,Wang,Liang-Liang,Zhang,Shuqun,et al. An efficient and concise synthesis of a selective small molecule non-peptide inhibitor of cathepsin L: KGP94[J]. BIOORGANIC CHEMISTRY,2021,116:105317. |
| APA | Munikishore,Rachakunta,Wang,Liang-Liang,Zhang,Shuqun,Zhao,Qin-Shi,&Zuo,Zhili.(2021).An efficient and concise synthesis of a selective small molecule non-peptide inhibitor of cathepsin L: KGP94.BIOORGANIC CHEMISTRY,116,105317. |
| MLA | Munikishore,Rachakunta,et al."An efficient and concise synthesis of a selective small molecule non-peptide inhibitor of cathepsin L: KGP94".BIOORGANIC CHEMISTRY 116(2021):105317. |
入库方式： OAI收割
来源：昆明植物研究所
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