Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8.

Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.

Bruncko M, McClellan WJ, Wendt MD, Sauer DR, Geyer A, Dalton CR, Kaminski MA, Weitzberg M, Gong J, Dellaria JF, Mantei R, Zhao X, Nienaber VL, Stewart K, Klinghofer V, Bouska J, Rockway TW, Giranda VL.

Source

Cancer Research, Global Pharmaceutical R&D, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6101, USA. milan.bruncko@abbott.com

Abstract

A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors.

PMID:: 15582418; [PubMed - indexed for MEDLINE]

MeSH Terms, Substances

MeSH Terms

Substances

LinkOut - more resources

Full Text Sources

Other Literature Sources

Labome Researcher Resource - ExactAntigen/Labome

Chemical Information

BindingDB

Supplemental Content

Save items

Related citations in PubMed

Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors. [Bioorg Med Chem Lett. 2004]
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.
Wendt MD, Geyer A, McClellan WJ, Rockway TW, Weitzberg M, Zhao X, Mantei R, Stewart K, Nienaber V, Klinghofer V, et al. Bioorg Med Chem Lett. 2004 Jun 21; 14(12):3063-8.
Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution. [J Med Chem. 2004]
Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.
Wendt MD, Rockway TW, Geyer A, McClellan W, Weitzberg M, Zhao X, Mantei R, Nienaber VL, Stewart K, Klinghofer V, et al. J Med Chem. 2004 Jan 15; 47(2):303-24.
Structure-directed discovery of potent non-peptidic inhibitors of human urokinase that access a novel binding subsite. [Structure. 2000]
Structure-directed discovery of potent non-peptidic inhibitors of human urokinase that access a novel binding subsite.
Nienaber VL, Davidson D, Edalji R, Giranda VL, Klinghofer V, Henkin J, Magdalinos P, Mantei R, Merrick S, Severin JM, et al. Structure. 2000 May 15; 8(5):553-63.
Review Structure, function and antagonists of urokinase-type plasminogen activator. [Front Biosci. 2009]
Review Structure, function and antagonists of urokinase-type plasminogen activator.
Vincenza Carriero M, Franco P, Vocca I, Alfano D, Longanesi-Cattani I, Bifulco K, Mancini A, Caputi M, Stoppelli MP. Front Biosci. 2009 Jan 1; 14:3782-94. Epub 2009 Jan 1.
Review Urokinase-type plasminogen activator. [Int J Biochem Cell Biol. 2007]
Review Urokinase-type plasminogen activator.
Crippa MP. Int J Biochem Cell Biol. 2007; 39(4):690-4. Epub 2006 Oct 21.

See reviews... See all...

Structures reported by this article

Substituted 2-naphthamadine Inhibitors Of Urokinase

PDB: 1U6Q

Source: Homo sapiens

Method: X-Ray Diffraction

Resolution: 2.02 Å

Related information

Related Citations
Calculated set of PubMed citations closely related to the selected article(s) retrieved using a word weight algorithm. Related articles are displayed in ranked order from most to least relevant, with the “linked from” citation displayed first.
BioAssay
PubChem BioAssay experiments on the biological activities of small molecules that cite the current articles. The depositors of BioAssay data provide these references.
Compound (MeSH Keyword)
PubChem chemical compound records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Substance (MeSH Keyword)
PubChem chemical substance (submitted) records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Taxonomy via GenBank
Taxonomy records associated with the current articles through taxonomic information on related molecular database records (Nucleotide, Protein, Gene, SNP, Structure).
Protein
Protein translation features of primary database (GenBank) nucleotide records reported in the current articles as well as Reference Sequences (RefSeqs) that include the articles as references.
Structure
Three-dimensional structure records in the NCBI Structure database for data reported in the current articles.

Recent activity

Clear Turn Off Turn On

Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacok...
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
Bioorg Med Chem Lett. 2005 Jan 3 ;15(1):93-8.

PubMed

Your browsing activity is empty.

Activity recording is turned off.

Turn recording back on

PubMed

Result Filters

Display Settings:

Send to: