Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 19, 2008, Pages 5255-5258

  Alper, Phil B ^a   Marsilje, Thomas H ^a   Mutnick, Daniel ^a   Lu, Wenshuo ^a   Chatterjee, Arnab ^a   Roberts, Michael J ^a   He, Yun ^a   Karanewsky, Donald S ^a   Chow, Donald ^a   Lao, Jianmin ^a   Gerken, Andrea ^a   Tuntland, Tove ^a   Liu, Bo ^a   Chang, Jonathan ^a   Gordon, Perry ^a   Martin Seidel, H ^a   Tian, Shin Shay ^a  

^a GENOMICS INSTITUTE OF THE NOVARTIS RESEARCH FOUNDATION   (United States)

Author keywords

Agonist; cMpl; Hematopoietic growth factor; Thrombopoietin; Tpo; TpoR

Indexed keywords

BENZENE DERIVATIVE; BENZO[A]CARBAZOLE DERIVATIVE; CARBAZOLE DERIVATIVE; ELTROMBOPAG; FIBRINOLYTIC AGENT; THROMBOPOIETIN RECEPTOR; TOTROMBOPAG; UNCLASSIFIED DRUG;

ARTICLE; DRUG BIOAVAILABILITY; DRUG HALF LIFE; DRUG POTENCY; DRUG SCREENING; HIGH THROUGHPUT SCREENING; HYDROPHOBICITY; MOUSE; NONHUMAN; STEREOSPECIFICITY; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; BENZENE DERIVATIVES; CARBAZOLES; COMBINATORIAL CHEMISTRY TECHNIQUES; DRUG DESIGN; HUMANS; MICE; MOLECULAR STRUCTURE; NUCLEAR MAGNETIC RESONANCE, BIOMOLECULAR; RECEPTORS, THROMBOPOIETIN; STRUCTURE-ACTIVITY RELATIONSHIP; THROMBOPOIETIN;

MUS;

EID: 52049096805     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.08.068     Document Type: Article

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27. 2 in acetic acid at 105 °C overnight. The final compounds are generated using standard synthetic methodology as described in Alper, P., et al. WO 2007/009120.
28. Prepared by treatment of 15 with LiOH at 150 °C for 10 min in a mixture of water and dioxane.
29. Formulated as a 2.5 mg/mL in PEG300/D5W (3:1) solution.