Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants

Journal of Medicinal Chemistry

Volumn 59, Issue 5, 2016, Pages 2005-2024

  Cheng, Hengmiao ^a   Nair, Sajiv K ^a   Murray, Brion W ^a   Almaden, Chau ^a   Bailey, Simon ^a   Baxi, Sangita ^a   Behenna, Doug ^a   Cho Schultz, Sujin ^a   Dalvie, Deepak ^a   Dinh, Dac M ^a   Edwards, Martin P ^a   Feng, Jun Li ^a   Ferre, Rose Ann ^a   Gajiwala, Ketan S ^a   Hemkens, Michelle D ^a   Jackson Fisher, Amy ^a   Jalaie, Mehran ^a   Johnson, Ted O ^a   Kania, Robert S ^a   Kephart, Susan ^a   Lafontaine, Jennifer ^a   Lunney, Beth ^a   Liu, Kevin K C ^a   Liu, Zhengyu ^a   Matthews, Jean ^a   Nagata, Asako ^a   Niessen, Sherry ^a   Ornelas, Martha A ^a   Orr, Suvi T M ^a   Pairish, Mason ^a   Planken, Simon ^a   Ren, Shijian ^b   Richter, Daniel ^a   Ryan, Kevin ^a   Sach, Neal ^a   Shen, Hong ^a   Smeal, Tod ^a   Solowiej, Jim ^a   Sutton, Scott ^a   Tran, Khanh ^a   Tseng, Elaine ^a   Vernier, William ^a   Walls, Marlena ^a   Wang, Shuiwang ^b   Weinrich, Scott L ^a   Xin, Shuibo ^b   Xu, Haiwei ^b   Yin, Min Jean ^a   Zientek, Michael ^a   Zhou, Ru ^a   Kath, John C ^a   more..

^a PFIZER INC   (United States)

^b WUXI APPTEC   (China)

Author keywords

[No Author keywords available]

Indexed keywords

1 [3 [[[5 CHLORO [(1 METHYL 1H PYRAZOL 4 YL)AMINO] 7H PYRROLO[2,3 D]PYRIMIDIN 4 YL]OXY]METHYL] 4 METHOXYPYRROLIDIN 1 YL]PROP 2 EN 1 ONE; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; MUTANT PROTEIN; PF 06459988; PROTEOME; UNCLASSIFIED DRUG; EGFR PROTEIN, HUMAN; PF-06459988; PROTEIN KINASE INHIBITOR; PYRIMIDINE DERIVATIVE; PYRROLE DERIVATIVE;

ARTICLE; BINDING AFFINITY; CHEMICAL REACTION; CONTROLLED STUDY; DRUG DESIGN; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG SPECIFICITY; DRUG SYNTHESIS; ENZYME INACTIVATION; ENZYME INHIBITION; GENE MUTATION; HUMAN; HUMAN CELL; LUNG CANCER CELL LINE; MOLECULAR DOCKING; NON SMALL CELL LUNG CANCER; PROTEIN DOMAIN; STRUCTURE ACTIVITY RELATION; WILD TYPE; ANTAGONISTS AND INHIBITORS; CARCINOMA, NON-SMALL-CELL LUNG; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG DEVELOPMENT; GENETICS; LUNG NEOPLASMS; MUTATION; SYNTHESIS; TUMOR CELL CULTURE;

CARCINOMA, NON-SMALL-CELL LUNG; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HUMANS; LUNG NEOPLASMS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; MUTANT PROTEINS; MUTATION; PROTEIN KINASE INHIBITORS; PYRIMIDINES; PYRROLES; RECEPTOR, EPIDERMAL GROWTH FACTOR; STRUCTURE-ACTIVITY RELATIONSHIP; TUMOR CELLS, CULTURED;

EID: 84960910347     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b01633     Document Type: Article

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