Literature DB >> 11738583

Potent P1' biphenylmethyl substituted aggrecanase inhibitors.

Wenqing Yao1, Michael Chao, Zelda R Wasserman, Rui Qin Liu, Maryanne B Covington, Robert Newton, David Christ, Ruth R Wexler, Carl P Decicco.   

Abstract

A series of cis-1(S)2(R)-amino-2-indanol based compounds with a biphenylmethyl group at the P1' position was found to be potent aggrecanase inhibitors. Both compounds 2j and 2n possessed very high aggrecanase affinity (IC(50)=1.5nM), and showed excellent selectivity over MMP-1 and MMP-9, with moderate selectivity against MMP-2.

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Year:  2002        PMID: 11738583     DOI: 10.1016/s0960-894x(01)00704-1

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


  4 in total

1.  Structural and inhibition analysis reveals the mechanism of selectivity of a series of aggrecanase inhibitors.

Authors:  Micky D Tortorella; Alfredo G Tomasselli; Karl J Mathis; Mark E Schnute; Scott S Woodard; Grace Munie; Jennifer M Williams; Nicole Caspers; Arthur J Wittwer; Anne-Marie Malfait; Huey-Sheng Shieh
Journal:  J Biol Chem       Date:  2009-07-08       Impact factor: 5.157

2.  Pharmacophore development and screening for discovery of potential inhibitors of ADAMTS-4 for osteoarthritis therapy.

Authors:  Priyanka Verma; Krishna Dalal; Madhu Chopra
Journal:  J Mol Model       Date:  2016-07-11       Impact factor: 1.810

3.  Screening of potential a disintegrin and metalloproteinase with thrombospondin motifs-4 inhibitors using a collagen model fluorescence resonance energy transfer substrate.

Authors:  Janelle L Lauer-Fields; Timothy P Spicer; Peter S Chase; Mare Cudic; Gayle D Burstein; Hideaki Nagase; Peter Hodder; Gregg B Fields
Journal:  Anal Biochem       Date:  2007-09-15       Impact factor: 3.365

Review 4.  Aggrecanases and cartilage matrix degradation.

Authors:  Hideaki Nagase; Masahide Kashiwagi
Journal:  Arthritis Res Ther       Date:  2003-02-14       Impact factor: 5.156

  4 in total

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