ChemMedChem p. 1776 - 1793 (2017)
Update date:2022-08-06
Topics:
Lücking, Ulrich
Scholz, Arne
Lienau, Philip
Siemeister, Gerhard
Kosemund, Dirk
Bohlmann, Rolf
Briem, Hans
Terebesi, Ildiko
Meyer, Kirstin
Prelle, Katja
Denner, Karsten
B?mer, Ulf
Sch?fer, Martina
Eis, Knut
Valencia, Ray
Ince, Stuart
von Nussbaum, Franz
Mumberg, Dominik
Ziegelbauer, Karl
Klebl, Bert
Choidas, Axel
Nussbaumer, Peter
Baumann, Matthias
Schultz-Fademrecht, Carsten
Rühter, Gerd
Eickhoff, Jan
Brands, Michael
Selective inhibition of exclusively transcription-regulating PTEFb/CDK9 is a promising new approach in cancer therapy. Starting from lead compound BAY-958, lead optimization efforts strictly focusing on kinase selectivity, physicochemical and DMPK properties finally led to the identification of the orally available clinical candidate atuveciclib (BAY 1143572). Structurally characterized by an unusual benzyl sulfoximine group, BAY 1143572 exhibited the best overall profile in vitro and in vivo, including high efficacy and good tolerability in xenograft models in mice and rats. BAY 1143572 is the first potent and highly selective PTEFb/CDK9 inhibitor to enter clinical trials for the treatment of cancer.
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