259796-12-8Relevant articles and documents
Preparation method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline
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Paragraph 0019-0020; 0026-0029; 0039-0041, (2021/02/06)
The invention provides a preparation method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline. The preparation method comprises the following steps: preparing a compound A by taking 3, 5-dichlorobenzoic acid as a raw material; preparing a compound B from the compound A; preparing a compound C from the compound B; preparing a compound D from the compound C; and obtaining a white solid 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline from the compound D. The preparation method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline provided by the invention has the advantages of high product purity and high product yield.
Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors
Kishore Kumar,Chavarria, Gustavo E.,Charlton-Sevcik, Amanda K.,Arispe, Wara M.,MacDonough, Matthew T.,Strecker, Tracy E.,Chen, Shen-En,Siim, Bronwyn G.,Chaplin, David J.,Trawick, Mary Lynn,Pinney, Kevin G.
supporting information; experimental part, p. 1415 - 1419 (2010/07/06)
A small library of 36 functionalized benzophenone thiosemicarbazone analogs has been prepared by chemical synthesis and evaluated for their ability to inhibit the cysteine proteases cathepsin L and cathepsin B. Inhibitors of cathepsins L and B have the potential to limit or arrest cancer metastasis. The six most active inhibitors of cathepsin L (IC50 50 > 10,000 nM). The most active analog in the series, 3-bromophenyl-2′-fluorophenyl thiosemicarbazone 1, also efficiently inhibits cell invasion of the DU-145 human prostate cancer cell line.
SUBSTITUTED PYRAZOLES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE
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Page/Page column 32, (2008/06/13)
The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes