About: Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors

Facets (new session)
Description
Metadata
Settings
- owl:sameAs
- Inference Rule:

About: Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors
Creator	Chen, Shen-En Arispe, Wara Chaplin, David Charlton-Sevcik, Amanda Chavarria, Gustavo Kishore Kumar, G Macdonough, Matthew Pinney, Kevin Siim, Bronwyn Strecker, Tracy Trawick, Mary
source	Elsevier; Medline; PMC
abstract	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 (IC(50) < 85 nM) in this series incorporate a meta-bromo substituent in one aryl ring along with a variety of functional groups in the second aryl ring. These six analogs are selective for their inhibition of cathepsin L versus cathepsin B (IC(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.
has issue date	2010-02-15(xsd:dateTime)
bibo:doi	10.1016/j.bmcl.2009.12.090
bibo:pmid	20089402
has license	no-cc
sha1sum (hex)	ae16a499f401dbae4849ba3da4d6a2f628ae209a
schema:url	https://doi.org/10.1016/j.bmcl.2009.12.090
resource representing a document's title	Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors
has PubMed Central identifier	PMC7125537
has PubMed identifier	20089402
schema:publication	Bioorg Med Chem Lett
resource representing a document's body	covid:ae16a499f401dbae4849ba3da4d6a2f628ae209a#body_text
is schema:about of	named entity 'variety' named entity 'series' named entity 'evaluated' named entity 'inhibits' named entity 'thiosemicarbazone' named entity 'ANALOG' named entity 'HAVE' named entity 'CYSTEINE PROTEASES' named entity 'ACTIVE' named entity 'THEIR' named entity 'LIMIT' named entity 'SECOND' named entity 'ARREST' named entity 'INHIBITORS' named entity 'HUMAN' named entity 'SERIES' named entity 'LIBRARY' named entity 'DU-145' named entity 'THIOSEMICARBAZONE' named entity '10%' named entity 'THESE' named entity 'RING' named entity 'THIOSEMICARBAZONE' named entity 'DESIGN' named entity 'PREPARED' named entity 'BROMO' named entity 'META' named entity 'CANCER METASTASIS' named entity 'CELL INVASION' named entity 'FUNCTIONAL GROUPS' named entity 'CATHEPSINS' named entity 'PROSTATE CANCER CELL LINE' named entity 'VARIETY' named entity 'BASED' named entity 'CATHEPSIN L INHIBITORS' named entity 'SYNTHESIS' named entity 'CATHEPSIN L' named entity 'CATHEPSIN B' named entity 'BENZOPHENONE' named entity 'TO INHIBIT' named entity 'INHIBITION' named entity 'BIOLOGICAL EVALUATION' named entity 'SMALL' named entity 'SUBSTITUENT' named entity 'CHEMICAL SYNTHESIS' named entity 'SELECTIVE' named entity 'EVALUATED' named entity 'ANALOGS' named entity 'POTENTIAL' covid:arg/ae16a499f401dbae4849ba3da4d6a2f628ae209a named entity 'inhibit' named entity 'inhibitors' named entity 'cathepsins' named entity 'cathepsin' named entity 'cathepsin' named entity 'cathepsin' named entity 'cathepsin' named entity 'cell line' named entity 'cysteine proteases' named entity 'Molecular modeling' named entity 'DU-145' named entity 'inhibitory activity' named entity 'peptide bonds' named entity 'preclinical studies' named entity 'chemical synthesis' named entity 'chemical synthesis' named entity 'analog' named entity 'moiety' named entity 'isomers' named entity 'HPLC' named entity 'cysteine proteases'

Faceted Search & Find service v1.13.91 as of Mar 24 2020

Alternative Linked Data Documents: Sponger | ODE Content Formats:

RDF

ODATA

Microdata

About

OpenLink Virtuoso version 07.20.3229 as of Jul 10 2020, on Linux (x86_64-pc-linux-gnu), Single-Server Edition (94 GB total memory)
Data on this page belongs to its respective rights holders.
Virtuoso Faceted Browser Copyright © 2009-2025 OpenLink Software