Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors

  • Bioorg Med Chem Lett. 2003 Dec 15;13(24):4365-9. doi: 10.1016/j.bmcl.2003.08.080.
Patrick Angibaud  1 ,  Xavier Bourdrez ,  David W End ,  Eddy Freyne ,  Michel Janicot ,  Patricia Lezouret ,  Yannick Ligny ,  Geert Mannens ,  Siegrid Damsch ,  Laurence Mevellec ,  Christophe Meyer ,  Philippe Muller ,  Isabelle Pilatte ,  Virginie Poncelet ,  Bruno Roux ,  Gerda Smets ,  Jacky Van Dun ,  Pieter Van Remoortere ,  Marc Venet ,  Walter Wouters
Affiliations
  • 1. Medicinal Chemistry Department Johnson & Johnson Pharmaceutical Research & Development (J&JPRD), Campus de Maigremont BP615, 27106, Val de Reuil, France. [email protected]
PMID: 14643327 DOI: 10.1016/j.bmcl.2003.08.080
Abstract

A series of (4-chlorophenyl)-alpha-(1-methyl-1H-imidazol-5-yl)azoloquinolines and -quinazolines was prepared. These compounds displayed potent Farnesyl Protein Transferase inhibitory activity and tetrazolo[1,5-a]quinazolines are promising agents for oral in vivo inhibition.