The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer

Journal of Medicinal Chemistry

Volumn 55, Issue 14, 2012, Pages 6523-6540

  Lewis, Richard T ^a   Bode, Christiane M ^a   Choquette, Deborah M ^a   Potashman, Michele ^a   Romero, Karina ^a   Stellwagen, John C ^a   Teffera, Yohannes ^a   Moore, Earl ^a   Whittington, Douglas A ^a   Chen, Hao ^a   Epstein, Linda F ^a   Emkey, Renee ^a   Andrews, Paul S ^a   Yu, Violeta L ^a   Saffran, Douglas C ^a   Xu, Man ^a   Drew, Allison ^a   Merkel, Patricia ^a   Szilvassy, Steven ^a   Brake, Rachael L ^a  

^a AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3,5 DIFLUORO N [6 [[4 (2 HYDROXYPROPAN 2 YL)PIPERIDIN 1 YL]METHYL] 1 [4 (ISOPROPYLCARBAMOYL)CYCLOHEXYL] 1H BENZO[D]IMIDAZOL 2(3H) YLIDENE]BENZAMIDE; 4 FLUORO N [6 [[4 (2 HYDROXYPROPAN 2 YL)PIPERIDIN 1 YL] METHYL] 1 [4 (ISOPROPYLCARBAMOYL)CYCLOHEXYL] 1H BENZO[D]IMIDAZOL 2(3H) YLIDENE]BENZAMIDE; ANAPLASTIC LYMPHOMA KINASE; PROTEIN TYROSINE KINASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CANCER THERAPY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG STRUCTURE; HUMAN; HUMAN CELL; NONHUMAN; PLASMA PROTEIN BINDING; RAT; STRUCTURE ACTIVITY RELATION; TUMOR REGRESSION;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; BIOLOGICAL AVAILABILITY; CELL LINE, TUMOR; DRUG DISCOVERY; DRUG STABILITY; HUMANS; IMIDAZOLES; INHIBITORY CONCENTRATION 50; MICROSOMES, LIVER; MODELS, MOLECULAR; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; RATS; RECEPTOR PROTEIN-TYROSINE KINASES; SUBSTRATE SPECIFICITY;

EID: 84864213321     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm3005866     Document Type: Article

References (22)

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17. Screen was performed by KINOMEscan, a division of DiscoveRx, 11180 Roselle Street, San Diego. CA 92121 USA; http://kinomescan.com/.
18. Screen was performed by Carna Biosciences. https://www.carnabio.com/ english/product/search.cgi?mode=profiling.
19. Details of additional studies will be reported elsewhere. In March 2011, Tesaro, Inc. signed an agreement with Amgen granting Tesaro exclusive worldwide rights for the development, manufacture, commercialization, and distribution of small molecule inhibitors of ALK. For more information, please contact Dr. Mary Lynne Hedley: MLHedley@tesarobio.com
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