287202-25-9Relevant articles and documents
Identification of potent and selective TACE inhibitors via the S1 pocket
Condon, Jeffrey S.,Joseph-McCarthy, Diane,Levin, Jeremy I.,Lombart, Henry-Georges,Lovering, Frank E.,Sun, Linhong,Wang, Weiheng,Xu, Weixin,Zhang, Yuhua
, p. 34 - 39 (2007/10/03)
By focusing on the P1 portion of the piperidine β-sulfone ligands we identified a motif that induces selectivity and resulted in a series of TACE inhibitors that demonstrated excellent in vitro potency against isolated TACE enzyme and excellent selectivity over MMPs 1, 2, 9, 13, and 14.
Design and synthesis of butynyloxyphenyl β-sulfone piperidine hydroxamates as TACE inhibitors
Park, Kaapjoo,Aplasca, Alexis,Du, Mila T.,Sun, LinHong,Zhu, Yi,Zhang, Yuhua,Levin, Jeremy I.
, p. 3927 - 3931 (2007/10/03)
A series of butynyloxyphenyl β-sulfone piperidine hydroxamate TACE inhibitors was designed and synthesized. The resulting structure-activity relationship and MMP selectivity of the series were examined. Of the compounds investigated, 17s has excellent in