Novel indole inhibitors of IMPDH from fragments: synthesis and initial structure-activity relationships

  • Bioorg Med Chem Lett. 2006 May 1;16(9):2539-42. doi: 10.1016/j.bmcl.2006.01.090.
Rebekah E Beevers  1 ,  George M Buckley ,  Natasha Davies ,  Joanne L Fraser ,  Francis C Galvin ,  Duncan R Hannah ,  Alan F Haughan ,  Kerry Jenkins ,  Stephen R Mack ,  William R Pitt ,  Andrew J Ratcliffe ,  Marianna D Richard ,  Verity Sabin ,  Andrew Sharpe ,  Sophie C Williams
Affiliations
  • 1. UCB Celltech, Granta Park, Great Abington, Cambridge, CB1 6GS, UK.
PMID: 16483773 DOI: 10.1016/j.bmcl.2006.01.090
Abstract

The elaboration of previously reported indole fragments as inhibitors of Inosine monophosphate dehydrogenase (IMPDH) is described. The synthesis, in vitro inhibitory values for IMPDH II, PBMC proliferation and physicochemical properties are discussed.