A Rhodium(III) Complex as an Inhibitor of Neural Precursor Cell Expressed, Developmentally Down-Regulated 8-Activating Enzyme with in Vivo Activity against Inflammatory Bowel Disease

J Med Chem. 2017 Jan 12;60(1):497-503. doi: 10.1021/acs.jmedchem.6b00250. Epub 2016 Dec 23.

Abstract

We report herein the identification of the rhodium(III) complex [Rh(phq)2(MOPIP)]+ (1) as a potent and selective ATP-competitive neural precursor cell expressed, developmentally down-regulated 8 (NEDD8)-activating enzyme (NAE) inhibitor. Structure-activity relationship analysis indicated that the overall organometallic design of complex 1 was important for anti-inflammatory activity. Complex 1 showed promising anti-inflammatory activity in vivo for the potential treatment of inflammatory bowel disease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Down-Regulation / drug effects*
  • Humans
  • NEDD8 Protein
  • Neural Stem Cells / enzymology*
  • Rhodium / chemistry*
  • Rhodium / pharmacology*
  • Structure-Activity Relationship
  • Ubiquitins / antagonists & inhibitors*

Substances

  • NEDD8 Protein
  • NEDD8 protein, human
  • Ubiquitins
  • Rhodium