Potent and selective cyclohexyl-derived imidazopyrazine insulin-like growth factor 1 receptor inhibitors with in vivo efficacy

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 4, 2011, Pages 1176-1180

  Jin, Meizhong ^a   Kleinberg, Andrew ^a   Cooke, Andy ^a   Gokhale, Prafulla C ^a   Foreman, Kenneth ^a   Dong, Hanqing ^a   Siu, Kam W ^a   Bittner, Mark A ^a   Mulvihill, Kristen M ^a   Yao, Yan ^a   Landfair, Darla ^a   O'Connor, Matthew ^a   Mak, Gilda ^a   Pachter, Jonathan A ^a   Wild, Robert ^a   Rosenfeld Franklin, Maryland ^a   Ji, Qunsheng ^a   Mulvihill, Mark J ^a  

^a OSI PHARMACEUTICALS INC   (United States)

Author keywords

Cancer; Inhibitors; Insulin like growth factor 1 receptor (IGF 1R); Tumor growth inhibition (TGI)

Indexed keywords

IMIDAZOPYRAZINE DERIVATIVE; PROTEIN TYROSINE KINASE INHIBITOR; QUINOLINE; SOMATOMEDIN C RECEPTOR;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CANCER INHIBITION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG METABOLISM; DRUG STRUCTURE; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; TUMOR XENOGRAFT;

ANIMALS; ANTINEOPLASTIC AGENTS; BENZIMIDAZOLES; IMIDAZOLES; MICE; NEOPLASMS; PROTEIN KINASE INHIBITORS; PYRAZINES; RECEPTOR, IGF TYPE 1; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSPLANTATION, HETEROLOGOUS;

EID: 79851513257     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.12.094     Document Type: Article

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18. 0 = median tumor volume of control group at time 0. Mean %TGI was calculated for the entire dosing period for each group. Significant anti-tumor activity is defined as mean %TGI >50%.