Design, Synthesis, and Evaluation of 3,5-Disubstituted 7-Azaindoles as Trk Inhibitors with Anticancer and Antiangiogenic Activities
摘要:
Tropomyosin-related kinase A (TrkA) is considered a promising target in the development of a therapeutic treatment of cancer and pain. In this study, we designed and synthesized a series of novel 7-azaindole-based Trk kinase inhibitors through the structure-based design strategy. By varying the functional groups at the 3 and 5 positions of a 7-azaindole scaffold, we studied the structure-activity relationships (SAR) profiles and identified a series of potent Trk inhibitors. Representative derivatives showed desirable activity in cellular proliferation and apoptosis assays. Moreover, these inhibitors exhibited noteworthy antiangiogenic activity.
[EN] 2- (QUINOXALIN-5-YLSULFONYLAMINO) -BENZAMIDE COMPOUNDS AS CCK2 MODULATORS<br/>[FR] COMPOSES DE 2- (QUINOXALINE-5-YLSULFONYLAMINO) -BENZAMIDE UTILISES EN TANT QUE MODULATEUR DU RECEPTEUR CCK2
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2005016896A1
公开(公告)日:2005-02-24
Certain amidophenyl-sulfonylamino-quinoxaline compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.