Literature DB >> 20846863

New non-hydroxamic ADAMTS-5 inhibitors based on the 1,2,4-triazole-3-thiol scaffold.

Lucie Maingot1, Florence Leroux, Valérie Landry, Julie Dumont, Hideaki Nagase, Bruno Villoutreix, Olivier Sperandio, Rebecca Deprez-Poulain, Benoit Deprez.   

Abstract

In this Letter we describe the design, synthesis, screening, and optimization of a new family of ADAMTS-5 inhibitors. These inhibitors display an original 1,2,4-triazole-3-thiol scaffold as a putative zinc binding-group. In vitro results are rationalized by in silico docking of the compounds in ADAMTS-5's crystal structure.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20846863     DOI： 10.1016/j.bmcl.2010.08.108

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


  7 in total

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Review 2.  Current and emerging therapeutic strategies for preventing inflammation and aggrecanase-mediated cartilage destruction in arthritis.

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Authors:  Ashraf A Aly; Stefan Bräse; Alaa A Hassan; Nasr K Mohamed; Lamiaa E Abd El-Haleem; Martin Nieger
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4.  Emerging Roles of ADAMTSs in Angiogenesis and Cancer.

Authors:  Saran Kumar; Nithya Rao; Ruowen Ge
Journal:  Cancers (Basel)       Date:  2012-11-29       Impact factor: 6.639

5.  Novel glyoxalase-I inhibitors possessing a "zinc-binding feature" as potential anticancer agents.

Authors:  Qosay A Al-Balas; Mohammad A Hassan; Nizar A Al-Shar'i; Nizar M Mhaidat; Ammar M Almaaytah; Fatima M Al-Mahasneh; Israa H Isawi
Journal:  Drug Des Devel Ther       Date:  2016-08-17       Impact factor: 4.162

6.  Generation of the first structure-based pharmacophore model containing a selective "zinc binding group" feature to identify potential glyoxalase-1 inhibitors.

Authors:  Qosay Al-Balas; Mohammad Hassan; Buthina Al-Oudat; Hassan Alzoubi; Nizar Mhaidat; Ammar Almaaytah
Journal:  Molecules       Date:  2012-11-22       Impact factor: 4.411

7.  Synthesis of a New Series of Nitrogen/Sulfur Heterocycles by Linking Four Rings: Indole; 1,2,4-Triazole; Pyridazine; and Quinoxaline.

Authors:  Ahmed T A Boraei; Ahmed A M Sarhan; Sammer Yousuf; Assem Barakat
Journal:  Molecules       Date:  2020-01-21       Impact factor: 4.411
  7 in total

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