Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine 790 → methionine 790 mutant

Journal of Medicinal Chemistry

Volumn 55, Issue 6, 2012, Pages 2711-2723

  Chang, Shaohua ^a,c   Zhang, Lianwen ^b,c   Xu, Shilin ^a,c   Luo, Jinfeng ^a   Lu, Xiaoyun ^a   Zhang, Zhang ^a   Xu, Tianfeng ^a,c   Liu, Yingxue ^a   Tu, Zhengchao ^a   Xu, Yong ^a   Ren, Xiaomei ^a   Geng, Meiyu ^d   Ding, Jian ^d   Pei, Duanqing ^a   Ding, Ke ^a  

^a INSTITUTE OF GEOLOGY AND GEOPHYSICS   (China)

^b UNIVERSITY OF SCIENCE AND TECHNOLOGY OF CHINA   (China)

^c UNIVERSITY OF CHINESE ACADEMY OF SCIENCES   (China)

^d SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; GEFITINIB; METHIONINE; N [3 [3 BENZYL 7 [2 METHOXY 4 (4 METHYLPIPERAZIN 1 YL) PHENYLAMINO] 2 OXO 3,4 DIHYDROPYRIMIDO[4,5 D]PYRIMIDIN 1(2H) YL]PHENYL]ACRYLAMIDE; N [3 [7 [2 METHOXY 4(4 METHYLPIPERAZIN 1 YL)PHENYLAMINO] 2 OXO 3 PHENYL 3,4 DIHYDROPYRIMIDO[4,5 D]PYRIMIDIN 1(2H) YL] PHENYL]ACRYLAMIDE; THREONINE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CANCER CELL; CELL PROLIFERATION; CONTROLLED STUDY; DRUG DESIGN; DRUG SCREENING; DRUG SYNTHESIS; ENZYME ACTIVITY; HUMAN; HUMAN CELL; IC 50; LUNG NON SMALL CELL CANCER; MOUSE; MUTANT; NONHUMAN; TUMOR XENOGRAFT; WESTERN BLOTTING;

ANIMALS; ANTINEOPLASTIC AGENTS; CARCINOMA, NON-SMALL-CELL LUNG; CELL PROLIFERATION; DRUG DESIGN; DRUG RESISTANCE, NEOPLASM; DRUG SCREENING ASSAYS, ANTITUMOR; HUMANS; LUNG NEOPLASMS; METHIONINE; MICE; MICE, NUDE; MICE, SCID; MOLECULAR CONFORMATION; MUTATION; NEOPLASM TRANSPLANTATION; PYRIMIDINES; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; STRUCTURE-ACTIVITY RELATIONSHIP; THREONINE; TRANSPLANTATION, HETEROLOGOUS;

EID: 84863341925     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm201591k     Document Type: Article

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