Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 15, 2012, Pages 4967-4974

  Peterson, Emily A ^a   Boezio, Alessandro A ^a   Andrews, Paul S ^a   Boezio, Christiane M ^a   Bush, Tammy L ^a   Cheng, Alan C ^a   Choquette, Deborah ^a   Coats, James R ^a   Colletti, Adria E ^a   Copeland, Katrina W ^a   Dupont, Michelle ^a   Graceffa, Russell ^a   Grubinska, Barbara ^a   Kim, Joseph L ^a   Lewis, Richard T ^a   Liu, Jingzhou ^a   Mullady, Erin L ^a   Potashman, Michele H ^a   Romero, Karina ^a   Shaffer, Paul L ^a   Stanton, Mary K ^a   Stellwagen, John C ^a   Teffera, Yohannes ^a   Yi, Shuyan ^a   Cai, Ti ^a   La, Daniel S ^a   more..

^a AMGEN INC   (United States)

Author keywords

Imidazopyridazine; Imidazopyridine; Kinase inhibitor; mTOR; Oncology

Indexed keywords

BENZIMIDAZOLE DERIVATIVE; EVEROLIMUS; IMIDAZOPYRIDAZINE DERIVATIVE; IMIDAZOPYRIDINE DERIVATIVE; MAMMALIAN TARGET OF RAPAMYCIN; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; PHOSPHATIDYLINOSITOL 3 KINASE; PROTEIN KINASE B; PYRIDAZINE DERIVATIVE; TEMSIROLIMUS; TRIAZINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CANCER CELL; CELL CYCLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BIOAVAILABILITY; DRUG DOSE COMPARISON; DRUG POTENCY; DRUG RESEARCH; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG TARGETING; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; GROWTH INHIBITION; HUMAN; HUMAN CELL; LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY; MOUSE; NONHUMAN; ONCOLOGY; RAT; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; TUMOR GROWTH;

ANIMALS; BENZIMIDAZOLES; BINDING SITES; BINDING, COMPETITIVE; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HALF-LIFE; HUMANS; IMIDAZOLES; MALE; MICE; MICROSOMES, LIVER; PHOSPHATIDYLINOSITOL 3-KINASES; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; PYRIDAZINES; PYRIDINES; RATS, SPRAGUE-DAWLEY; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP; TOR SERINE-THREONINE KINASES;

EID: 84863985849     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.06.033     Document Type: Article

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