Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 12, 2011, Pages 3743-3748

  Thomas, Mathew ^a   Huang, Wei Sheng ^a   Wen, David ^a   Zhu, Xiaotian ^a   Wang, Yihan ^a   Metcalf, Chester A ^a   Liu, Shuangying ^a   Chen, Ingrid ^a   Romero, Jan ^a   Zou, Dong ^a   Sundaramoorthi, Raji ^a   Li, Feng ^a   Qi, Jiwei ^a   Cai, Lisi ^a   Zhou, Tianjun ^a   Commodore, Lois ^a   Xu, Qihong ^a   Keats, Jeff ^a   Wang, Frank ^a   Wardwell, Scott ^a   Ning, Yaoyu ^a   Snodgrass, Joseph T ^a   Broudy, Marc I ^a   Russian, Karin ^a   Iuliucci, John ^a   Rivera, Victor M ^a   Sawyer, Tomi K ^a   Dalgarno, David C ^a   Clackson, Tim ^a   Shakespeare, William C ^a   more..

^a ARIAD PHARMACEUTICALS INC   (United States)

Author keywords

BCR ABL inhibitors; Chronic myeloid leukemia; Gatekeeper mutant; Monocycles; Ponatinib

Indexed keywords

BCR ABL PROTEIN; PONATINIB; PROTEIN TYROSINE KINASE INHIBITOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CHRONIC MYELOID LEUKEMIA; CONTROLLED STUDY; DRUG DISTRIBUTION; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; IC 50; MOUSE; MUTANT; NONHUMAN; RAT;

ADMINISTRATION, ORAL; ALKYNES; ANILINE COMPOUNDS; ANIMALS; CYCLIZATION; DISEASE MODELS, ANIMAL; FUSION PROTEINS, BCR-ABL; LEUKEMIA, MYELOGENOUS, CHRONIC, BCR-ABL POSITIVE; MICE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; MUTATION; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; TOLUENE;

PYRONIA TITHONUS;

EID: 79957857223     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.04.060     Document Type: Article

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