Literature DB >> 15149645

Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.

Michael D Wendt1, Andrew Geyer, William J McClellan, Todd W Rockway, Moshe Weitzberg, Xumiao Zhao, Robert Mantei, Kent Stewart, Vicki Nienaber, Vered Klinghofer, Vincent L Giranda.   

Abstract

Several 8-substituted 2-naphthamidine-based inhibitors of the serine protease urokinase plasminogen activator (uPA) are described. Direct attachment of five-membered saturated or unsaturated rings improved inhibitor performance; substitution with sulfones further improved binding profiles. Combination of these substituents or of previously described NH-linked heteroaromatic rings with 6-phenyl amide substituents provided further enhancements to potency and selectivity.

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Year:  2004        PMID： 15149645     DOI： 10.1016/j.bmcl.2004.04.030

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  7 in total

1.  Discovery and Design of First Benzylamine-Based Ligands Binding to an Unlocked Conformation of the Complement Factor D.

Authors:  Anna Vulpetti; Nils Ostermann; Stefan Randl; Taeyoung Yoon; Aengus Mac Sweeney; Frederic Cumin; Edwige Lorthiois; Simon Rüdisser; Paul Erbel; Jürgen Maibaum
Journal:  ACS Med Chem Lett       Date:  2018-04-24       Impact factor: 4.345

2.  Discovery of novel urokinase plasminogen activator (uPA) inhibitors using ligand-based modeling and virtual screening followed by in vitro analysis.

Authors:  Mahmoud A Al-Sha'er; Mohammad A Khanfar; Mutasem O Taha
Journal:  J Mol Model       Date:  2014-01-28       Impact factor: 1.810

3.  Challenging the gold standard for 3D-QSAR: template CoMFA versus X-ray alignment.

Authors:  Bernd Wendt; Richard D Cramer
Journal:  J Comput Aided Mol Des       Date:  2014-06-17       Impact factor: 3.686

4.  6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.

Authors:  Benjamin J Buckley; Ashraf Aboelela; Elahe Minaei; Longguang X Jiang; Zhihong Xu; Umar Ali; Karen Fildes; Chen-Yi Cheung; Simon M Cook; Darren C Johnson; Daniel A Bachovchin; Gregory M Cook; Minoti Apte; Mingdong Huang; Marie Ranson; Michael J Kelso
Journal:  J Med Chem       Date:  2018-09-07       Impact factor: 7.446

Review 5.  Urokinase plasminogen activator as an anti-metastasis target: inhibitor design principles, recent amiloride derivatives, and issues with human/mouse species selectivity.

Authors:  Nehad S El Salamouni; Benjamin J Buckley; Marie Ranson; Michael J Kelso; Haibo Yu
Journal:  Biophys Rev       Date:  2022-01-06

6.  Discovery of novel 5-fluoro-N2,N4-diphenylpyrimidine-2,4-diamines as potent inhibitors against CDK2 and CDK9.

Authors:  Jiadi Gao; Cheng Fang; Zhiyan Xiao; Li Huang; Chin-Ho Chen; Li-Ting Wang; Kuo-Hsiung Lee
Journal:  Medchemcomm       Date:  2015-03-01       Impact factor: 3.597

Review 7.  Proteolysis is the most fundamental property of malignancy and its inhibition may be used therapeutically (Review).

Authors:  Marzena Wyganowska-Świątkowska; Mateusz Tarnowski; Daniel Murtagh; Ewa Skrzypczak-Jankun; Jerzy Jankun
Journal:  Int J Mol Med       Date:  2018-11-07       Impact factor: 4.101
  7 in total

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