Novel pyrazolopyrimidines as highly potent B-Raf inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 24, 2009, Pages 6957-6961

  Di Grandi, Martin J ^a   Berger, Dan M ^a   Hopper, Darrin W ^a   Zhang, Chunchun ^a   Dutia, Minu ^a   Dunnick, Alejandro L ^a   Torres, Nancy ^a   Levin, Jeremy I ^a   Diamantidis, George ^a   Zapf, Christoph W ^a   Bloom, Jonathan D ^a   Hu, YongBo ^a   Powell, Dennis ^a   Wojciechowicz, Donald ^a   Collins, Karen ^a   Frommer, Eileen ^a  

^a WYETH RESEARCH   (United States)

Author keywords

B Raf; B Raf inhibitors; Indazole; Phenol isostere; Pyrazolopyrimidines

Indexed keywords

ANTINEOPLASTIC AGENT; B RAF KINASE; B RAF KINASE INHIBITOR; PYRAZOLOPYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER CELL CULTURE; CELL PROLIFERATION; CELL STRAIN A375; CELL STRAIN WM266; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DRUG POTENCY; HUMAN; HUMAN CELL; STRUCTURE ACTIVITY RELATION;

ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; CELL PROLIFERATION; ENZYME INHIBITORS; HUMANS; PROTO-ONCOGENE PROTEINS B-RAF; PYRAZOLES; PYRIDINES; PYRIMIDINES;

EID: 71849090215     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.10.058     Document Type: Article

References (20)

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20. Compound 4p had a therapeutic index of 9.4 and 19.3 for A375 and WM266 cells, respectively, and compound 4r had indices of 5.8 and 12, respectively; see Ref. 15.