Planta Med 2012; 78 - PD33
DOI: 10.1055/s-0032-1320391

Versatile selective kinase inhibitors: Chemistry and biology of indirubins

N Gaboriaud-Kolar 1, P Magiatis 1, A Brivanlou 2, P Greengard 3, S Knapp 4, S Nam 5, R Jove 5, L Meijer 6, E Mikros 1, AL Skaltsounis 1
  • 1Departments of Pharmacognosy and Pharmaceutical Chemistry, School of Pharmacy, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771, Athens, Greece
  • 2Laboratory of Molecular Vertebrate Embryology
  • 3Laboratory of Molecular and Cellular Neuroscience, The Rockfeller University, 1230 York Avenue, New-York, NY10065, USA
  • 4Nuffield Department of Clinical Medicine, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Headington, Oxford, OX37DQ, UK
  • 5Molecular Medicine Beckman Research Institute, City of Hope Comprehensive Cancer Center, 1500 East Duarte Road, Duarte, California, 91010, USA
  • 6Cell Cycle Group, Station Biologique de Roscoff, BP 74 29682 Roscoff Cedex, France

In an effort to identify new kinases inhibitors, natural and synthetic indirubins have been tested. This full SAR study led to the discovery of versatile selective kinases inhibitors according to the substitutions degree. This inhibition selectivity led to diverse biological activities e.g. stem cell pluripotency preservation1 or in vivo anti-tumor activities.

1: N. Sato et al, Nature Med, 2004, 10, 55–63.