Literature DB >> 17188863

Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

James E Sheppeck1, John L Gilmore, Anle Yang, Xiao-Tao Chen, Chu-Biao Xue, John Roderick, Rui-Qin Liu, Maryanne B Covington, Carl P Decicco, James J-W Duan.   

Abstract

A series of novel hydantoins was designed and synthesized as structural alternatives to hydroxamate inhibitors of TACE. 5-Mono- and di-substituted hydantoins exhibited activity with IC50 values of 11-60 nM against porcine TACE in vitro and excellent selectivity against other MMPs.

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Year:  2006        PMID： 17188863     DOI： 10.1016/j.bmcl.2006.11.089

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


  3 in total

1.  Development of predictive pharmacophore model for in silico screening, and 3D QSAR CoMFA and CoMSIA studies for lead optimization, for designing of potent tumor necrosis factor alpha converting enzyme inhibitors.

Authors:  Prashant Revan Murumkar; Vishal Prakash Zambre; Mange Ram Yadav
Journal:  J Comput Aided Mol Des       Date:  2010-02-24       Impact factor: 3.686

Review 2.  Targeting Metalloenzymes for Therapeutic Intervention.

Authors:  Allie Y Chen; Rebecca N Adamek; Benjamin L Dick; Cy V Credille; Christine N Morrison; Seth M Cohen
Journal:  Chem Rev       Date:  2018-09-07       Impact factor: 60.622

Review 3.  5-Ene-4-thiazolidinones - An efficient tool in medicinal chemistry.

Authors:  Danylo Kaminskyy; Anna Kryshchyshyn; Roman Lesyk
Journal:  Eur J Med Chem       Date:  2017-09-20       Impact factor: 6.514
  3 in total

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