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10.1002/cmdc.201700447

http://scihub22266oqcxt.onion/10.1002/cmdc.201700447
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C5698704!5698704!28961375
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suck abstract from ncbi


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pmid28961375      ChemMedChem 2017 ; 12 (21): 1776-93
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  • Identification of Atuveciclib (BAY?1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer #MMPMID28961375
  • Lücking U; Scholz A; Lienau P; Siemeister G; Kosemund D; Bohlmann R; Briem H; Terebesi I; Meyer K; Prelle K; Denner K; Bömer U; Schäfer M; Eis K; Valencia R; Ince S; von?Nussbaum F; Mumberg D; Ziegelbauer K; Klebl B; Choidas A; Nussbaumer P; Baumann M; Schultz?Fademrecht C; Rühter G; Eickhoff J; Brands M
  • 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.
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