Recent progress on third generation covalent EGFR inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 26, Issue 8, 2016, Pages 1861-1868

  Cheng, Hengmiao ^a   Nair, Sajiv K ^a   Murray, Brion W ^a  

^a PFIZER INC   (United States)

Author keywords

Covalent inhibitor; Drug resistance; EGFR; Lung cancer; NSCLC; Oncogenic mutation; SBDD; T790M

Indexed keywords

ASP 8273; AZ 5104; AZ 7550; EGF 816; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; HM 61713; OSIMERTINIB; PF 06747775; ROCILETINIB; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; EPIDERMAL GROWTH FACTOR RECEPTOR; PROTEIN KINASE INHIBITOR;

ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; CANCER CHEMOTHERAPY; CANCER INHIBITION; CANCER RESISTANCE; COVALENT BOND; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DEVELOPMENT; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG SAFETY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG TOLERABILITY; HUMAN; IC50; IN VITRO STUDY; LUNG CANCER; MUTANT; NON SMALL CELL LUNG CANCER; NONHUMAN; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); TREATMENT RESPONSE; TUMOR XENOGRAFT; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG EFFECTS; DRUG RESISTANCE; ENZYMOLOGY; GENETICS; METABOLISM; NEOPLASMS;

ANIMALS; ANTINEOPLASTIC AGENTS; DRUG RESISTANCE, NEOPLASM; HUMANS; NEOPLASMS; PROTEIN KINASE INHIBITORS; RECEPTOR, EPIDERMAL GROWTH FACTOR;

EID: 84960984325     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2016.02.067     Document Type: Review

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