SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 5, 2010, Pages 1744-1748

  Zimmermann, Kurt ^a   Wittman, Mark D ^a   Saulnier, Mark G ^a   Velaparthi, Upender ^a   Sang, Xiaopeng ^a   Frennesson, David B ^a   Struzynski, Charles ^a   Seitz, Steven P ^a   He, Liqi ^a   Carboni, Joan M ^a   Li, Aixin ^a   Greer, Ann F ^a   Gottardis, Marco ^a   Attar, Ricardo M ^b   Yang, Zheng ^a   Balimane, Praveen ^a   Discenza, Lorell N ^a   Lee, Francis Y ^a   Sinz, Michael ^a   Kim, Sean ^a   Vyas, Dolatrai ^a   more..

^a BRISTOL MYERS SQUIBB   (United States)

^b CENTOCOR INC   (United States)

Author keywords

CYP3A expression; Cytochrome P450; IGF 1R; Insulin like Growth Factor 1 Receptor kinase; Pregnane X receptor; PXR; PXR transactivation; SAR

Indexed keywords

3 (BENZIMIDAZOL 2 YL) PYRIDINE 2 ONE; ADENOSINE TRIPHOSPHATE; ANTINEOPLASTIC AGENT; BENZIMIDAZOLE DERIVATIVE; CYTOCHROME P450 3A4; MORPHOLINE; PHOSPHOTRANSFERASE INHIBITOR; PREGNANE X RECEPTOR; RIFAMPICIN; SOMATOMEDIN C RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CANCER INHIBITION; DRUG EXPOSURE; DRUG METABOLISM; DRUG PROTEIN BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; IC 50; IN VIVO STUDY; LIGAND BINDING; LIPOPHILICITY; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; TRANSACTIVATION; TUMOR XENOGRAFT;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; BENZIMIDAZOLES; CELL LINE, TUMOR; CYTOCHROME P-450 CYP3A; HUMANS; MICE; MICE, NUDE; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; RECEPTOR, IGF TYPE 1; RECEPTORS, STEROID; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSCRIPTIONAL ACTIVATION; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 76649090591     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.01.087     Document Type: Article

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