Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 10, 2010, Pages 3182-3185

  Velaparthi, Upender ^a   Saulnier, Mark G ^a   Wittman, Mark D ^a   Liu, Peiying ^a   Frennesson, David B ^a   Zimmermann, Kurt ^a   Carboni, Joan M ^a   Gottardis, Marco ^a   Li, Aixin ^a   Greer, Ann ^a   Clarke, Wendy ^a   Yang, Zheng ^a   Menard, Krista ^a   Lee, Francis Y ^a   Trainor, George ^a   Vyas, Dolatrai ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

Benzimidazole; CYP3A4 inhibition; IGF; Insulin like growth factor 1 receptor (IGF 1R); Kinases; Piperazine; Solubility

Indexed keywords

3 [6 (4 SUBSTITUTED PIPERAZIN 1 YL) 4 METHYL 1H BENZIMIDAZOL 2 YL] 1H PYRIMIDINE 2 ONE; AMIDE; ANTINEOPLASTIC AGENT; BMS 536924; BMS 577098; CARBAMIC ACID DERIVATIVE; CYTOCHROME P450 3A4; PIPERAZINE DERIVATIVE; SOMATOMEDIN RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; COLON CARCINOMA; CONTROLLED STUDY; DRUG DETERMINATION; DRUG EFFICACY; DRUG IDENTIFICATION; DRUG METABOLISM; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SOLUBILITY; ENZYME INHIBITION; IN VIVO STUDY; MOUSE; NONHUMAN; RAT; RHABDOMYOSARCOMA; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; BENZIMIDAZOLES; CYTOCHROME P-450 CYP3A; HUMANS; MICE; MICE, NUDE; PIPERAZINES; PROTEIN KINASE INHIBITORS; PYRIDONES; RATS; RECEPTOR, IGF TYPE 1; STRUCTURE-ACTIVITY RELATIONSHIP; XENOGRAFT MODEL ANTITUMOR ASSAYS;

ANIMALIA;

EID: 77952110655     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.03.057     Document Type: Article

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