62810-50-8Relevant academic research and scientific papers
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
, (2021/09/06)
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.
COMPOSITIONS AND METHODS FOR INHIBITION OF CATHEPSINS
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, (2017/03/14)
This present disclosure is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin L, cathepsin K, and/or cathepsin B, will be therapeutically useful.
Synthesis and biological evaluation of a water-soluble phosphate prodrug salt and structural analogues of KGP94, a lead inhibitor of cathepsin L
Parker, Erica N.,Odutola, Samuel O.,Wang, Yifan,Strecker, Tracy E.,Mukherjee, Rajeswari,Shi, Zhe,Chaplin, David J.,Trawick, Mary Lynn,Pinney, Kevin G.
, p. 1304 - 1310 (2017/06/19)
The magnitude of expression of cathepsin L, often upregulated in the tumor microenvironment, correlates with the invasive and metastatic nature of certain tumors. Inhibition of cathepsin L represents an emerging strategy for the treatment of metastatic ca
