4-Substituted-2-phenylquinazolines as inhibitors of BCRP

  • Bioorg Med Chem Lett. 2012 Nov 1;22(21):6766-9. doi: 10.1016/j.bmcl.2012.08.024.
Kapil Juvale  1 ,  Michael Wiese
Affiliations
  • 1. Pharmaceutical Institute, University of Bonn, Pharmaceutical Chemistry II, An der Immenburg 4, 53121 Bonn, Germany.
PMID: 23017888 DOI: 10.1016/j.bmcl.2012.08.024
Abstract

We investigated several 2-phenylquinazolines with different substitutions at position 4 for their BCRP inhibition. Compounds with phenyl ring attached via an amine-containing linker at position 4 were found to be potent inhibitors of BCRP. In general compounds with meta substitution of phenyl ring at position 4 were found to have higher inhibitory effect, compound 12 being the most potent and selective towards BCRP.