Literature DB >> 15177467

Synthesis and evaluation of aminophosphinic acid derivatives as inhibitors of renal dipeptidase.

Hallur Gurulingappa1, Phillip Buckhalts, Kenneth W Kinzler, Bert Vogelstein, Saeed R Khan.   

Abstract

Renal dipeptidase (RDP) is an enzyme overexpressed in benign and malignant colorectal tumors. In an effort to identify potent inhibitors of this enzyme, a series of aminophosphinic acid derivatives were synthesized. Compounds 3a and 3c in which the phenyl ring was para substituted with F and Br and olefin with Z geometry, showed better inhibitory activity against RDP enzyme (IC50 = 5-6 nM).

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Year:  2004        PMID: 15177467     DOI: 10.1016/j.bmcl.2004.04.057

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


  1 in total

Review 1.  Synthesis and modifications of phosphinic dipeptide analogues.

Authors:  Artur Mucha
Journal:  Molecules       Date:  2012-11-15       Impact factor: 4.411

  1 in total

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