Design, synthesis and biological evaluation of pyrazolyl-thiazolinone derivatives as potential EGFR and HER-2 kinase inhibitors

Bioorganic and Medicinal Chemistry

Volumn 20, Issue 6, 2012, Pages 2010-2018

  Qiu, Ke Ming ^a   Wang, Hai Hong ^a   Wang, Li Ming ^a   Luo, Yin ^a   Yang, Xian Hui ^a   Wang, Xiao Ming ^a   Zhu, Hai Liang ^a  

^a NANJING UNIVERSITY   (China)

Author keywords

Antitumor; EGFR; HER 2; Pyrazolyl thiazolidinone; Structure activity relationship

Indexed keywords

2 (3,5 DIPHENYL 4,5 DIHYDRO 1H PYRAZOL 1 YL)THIAZOL 4(5H)ONE; 2 (5 PHENYL 3 4 TOLYL 4,5 DIHYDRO 1H PYRAZOL 1 YL)THIAZOL 4(5H)ONE; 2 [3 (4 BROMOPHENYL) 5 (4 CHLOROPHENYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3 (4 BROMOPHENYL) 5 (4 FLUOROPHENYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3 (4 BROMOPHENYL) 5 (4 METHOXYPHENYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3 (4 BROMOPHENYL) 5 PHENYL 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3 (4 CHLOROPHENYL) 5 (4 FLUOROPHENYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3 (4 CHLOROPHENYL) 5 (4 METHOXYPHENYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3 (4 CHLOROPHENYL) 5 (4 TOLYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3 (4 CHLOROPHENYL) 5 PHENYL 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3 (4 FLUOROPHENYL) 5 (4 METHOXYPHENYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3 (4 FLUOROPHENYL) 5 (4 TOLYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3 (4 FLUOROPHENYL) 5 PHENYL 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3 PHENYL 5 (4 TOLYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3,5 BIS(4 BROMOPHENYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3,5 BIS(4 CHLOROPHENYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [3,5 BIS(4 FLUOROPHENYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [5 (4 BROMOPHENYL) 3 (4 CHLOROPHENYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [5 (4 BROMOPHENYL) 3 (4 FLUOROPHENYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [5 (4 BROMOPHENYL) 3 PHENYL 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [5 (4 CHLOROPHENYL) 3 (4 FLUOROPHENYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [5 (4 CHLOROPHENYL) 3 (4 TOLYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [5 (4 CHLOROPHENYL) 3 PHENYL 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [5 (4 FLUOROPHENYL) 3 (4 TOLYL) 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [5 (4 FLUOROPHENYL) 3 PHENYL 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; 2 [5 (4 METHOXYPHENYL) 3 PHENYL 4,5 DIHYDRO 1H PYRAZOL 1 YL]THIAZOL 4(5H)ONE; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; PYRAZOLYL THIAZOLINONE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; ARTICLE; CANCER CELL CULTURE; CELL STRAIN B16 F10; CELL STRAIN HCT116; CELL STRAIN MCF 7; CONTROLLED STUDY; DRUG DESIGN; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; ENZYME ACTIVE SITE; ENZYME INHIBITION; IC 50; IN VITRO STUDY; MOLECULAR DOCKING; STRUCTURE ACTIVITY RELATION;

ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; DRUG DESIGN; DRUG SCREENING ASSAYS, ANTITUMOR; HUMANS; MODELS, MOLECULAR; NEOPLASMS; PROTEIN KINASE INHIBITORS; RECEPTOR, EPIDERMAL GROWTH FACTOR; RECEPTOR, ERBB-2;

EID: 84862819626     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2012.01.051     Document Type: Article

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