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

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

Research output: Contribution to journalArticle

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 (IC 50=5-6nM).

Original languageEnglish (US)
Pages (from-to)3531-3533
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number13
DOIs
StatePublished - Jul 5 2004

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dipeptidase 1
Derivatives
Acids
Alkenes
Enzyme Inhibitors
Enzymes
Tumors
Colorectal Neoplasms
Geometry

Keywords

  • Aminophosphinic acid derivatives
  • RDP inhibitors

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Synthesis and evaluation of aminophosphinic acid derivatives as inhibitors of renal dipeptidase. / Gurulingappa, Hallur; Buckhalts, Phillip; Kinzler, Kenneth W; Vogelstein, Bert; Khan, Saeed R.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 14, No. 13, 05.07.2004, p. 3531-3533.

Research output: Contribution to journalArticle

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