An efficient and concise synthesis of a selective small molecule non-peptide inhibitor of cathepsin L: KGP94

doi:10.1016/j.bioorg.2021.105317

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	An efficient and concise synthesis of a selective small molecule non-peptide inhibitor of cathepsin L: KGP94
	Munikishore,Rachakunta ; Wang,Liang-Liang ; Zhang,Shuqun ; Zhao,Qin-Shi ; Zuo,Zhili
	2021
发表期刊	BIOORGANIC CHEMISTRY
ISSN	0045-2068
卷号	116 页码:105317
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.
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
DOI	10.1016/j.bioorg.2021.105317
WOS记录号	WOS:000701702300006
引用统计
文献类型	期刊论文
条目标识符	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.[Munikishore, Rachakunta 2.Wang, Liang-Liang 3.Zhang, Shuqun 4.Zhao, Qin-Shi 5.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China
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.

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