Fragment-based discovery of new highly substituted 1 H-pyrrolo [2, 3-b]-and 3 H-imidazolo [4, 5-b]-pyridines as focal adhesion kinase inhibitors

T Heinrich, J Seenisamy, L Emmanuvel…

Index: Heinrich, Timo; Seenisamy, Jeyaprakashnarayanan; Emmanuvel, Lourdusamy; Kulkarni, Santosh S.; Bomke, Joerg; Rohdich, Felix; Greiner, Hartmut; Esdar, Christina; Krier, Mireille; Graedler, Ulrich; Musil, Djordje Journal of Medicinal Chemistry, 2013 , vol. 56, # 3 p. 1160 - 1170

Full Text: HTML

Citation Number: 22

Abstract

Focal adhesion kinase (FAK) is considered as an attractive target for oncology, and small- molecule inhibitors are reported to be in clinical testing. In a surface plasmon resonance (SPR)-mediated fragment screening campaign, we discovered bicyclic scaffolds like 1 H- pyrazolo [3, 4-d] pyrimidines binding to the hinge region of FAK. By an accelerated knowledge-based fragment growing approach, essential pharmacophores were added. ...