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Deprecated: Implicit conversion from float 267.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 ChemMedChem 2017 ; 12 (21): 1776-93 Nephropedia Template TP
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Identification of Atuveciclib (BAY?1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer #MMPMID28961375
ChemMedChem 2017[Nov]; 12 (21): 1776-93 PMID28961375show ga
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.