2. Academic Validation
  3. Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors

Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors

  • ACS Med Chem Lett. 2014 Oct 23;6(1):73-8. doi: 10.1021/ml5003376.
Nis Halland 1,  Friedemann Schmidt 1,  Tilo Weiss 1,  Joachim Saas 1,  Ziyu Li 1,  Jörg Czech 1,  Matthias Dreyer 1,  Armin Hofmeister 1,  Katharina Mertsch 1,  Uwe Dietz 1,  Carsten Strübing 1,  Marc Nazare 2
Affiliations

Affiliations

  • 1 Sanofi R&D , Industriepark Höchst Building G838, D-65926 Frankfurt am Main, Germany.
  • 2 Leibniz-Institut für Molekulare Pharmakologie (FMP) , Robert-Rössle-Straße 10, 13125 Berlin-Buch, Germany.
PMID: 25589934 DOI: 10.1021/ml5003376
Abstract

From a virtual screening starting point, inhibitors of the serum and glucocorticoid regulated kinase 1 were developed through a combination of classical medicinal chemistry and library approaches. This resulted in highly active small molecules with nanomolar activity and a good overall in vitro and ADME profile. Furthermore, the compounds exhibited unusually high kinase and off-target selectivity due to their rigid structure.

Keywords

AGC kinase; Serum glucocorticoid regulated kinase; WNT signaling; virtual screening.

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