Synthesis, preliminary biological evaluation and molecular modeling of some new heterocyclic inhibitors of TACE

Central heteroaryl ring analogues belonging to a series of potent hydroxamate TACE inhibitors were synthesized. The TACE inhibitory activities of these compounds were evaluated by in vitro WBA and in silico molecular modeling studies using crystal structure of human TACE. Compound 14 showed very good in vitro inhibition, supported by the in silico docking studies. (C) 2011 Elsevier Masson SAS. All rights reserved.