The Pyrazolobenzothiazine Core as a New Chemotype of p38 Alpha Mitogen-Activated Protein Kinase Inhibitors
Stefano Sabatini, Giuseppe Manfroni, Maria Letizia Barreca, Silke M. Bauer, Marco Gargaro, Rolando Cannalire, Andrea Astolfi, Jose Brea, Carmine Vacca, Matteo Pirro, Serena Massari, Oriana Tabarrini, Maria Isabel Loza, Francesca Fallarino, Stefan A. Laufer and Violetta Cecchetti
Article first published online: 19 FEB 2015 | DOI: 10.1111/cbdd.12516
A series of pyrazolobenzothiazines has been identified as novel p38α MAPK inhibitors. Hit compound 6 turned out to be an effective inhibitor with a reasonable kinase selectivity profile. The obtained results strongly indicate the pyrazolobenzothiazine core as a new p38α inhibitor chemotype worthy of hit-to-lead optimization work.