Discovery and development of pyrazole-scaffold Hsp90 inhibitors

Current Topics in Medicinal Chemistry

Volumn 6, Issue 11, 2006, Pages 1193-1203

  McDonald, Edward ^a   Jones, Keith ^a   Brough, Paul A ^b   Drysdale, Martin J ^b   Workman, Paul ^a  

^a INSTITUTE OF CANCER RESEARCH   (United Kingdom)

^b Vernalis PLC   (United Kingdom)

Author keywords

ATP binding domain; Cyclin dependent kinase 4; Geldanamycin; Pyrazole scaffold; Structure activity relationship; Time resolved fluorescence resonance

Indexed keywords

17 ALLYLAMINO 17 DEMETHOXYGELDANAMYCIN; 17 DIMETHYLAMINOETHYL 17 DEMETHOXYGELDANAMYCIN; ADENOSINE TRIPHOSPHATASE; AMIDE; ANSAMYCIN DERIVATIVE; ANTINEOPLASTIC AGENT; BCR ABL PROTEIN; BENZENE DERIVATIVE; CCT 018159; CCT 074897; CCT 08159; CCT 129397; CHAPERONE; CYCLIN DEPENDENT KINASE 4; EPIDERMAL GROWTH FACTOR RECEPTOR 2; G 3129; G 3130; GELDANAMYCIN; HEAT SHOCK PROTEIN 90; HEAT SHOCK PROTEIN 90 INHIBITOR; IPI 504; ISOXAZOLE DERIVATIVE; NATURAL PRODUCT; PIPERAZINE DERIVATIVE; PROTEIN INHIBITOR; PYRAZOLE DERIVATIVE; RADICICOL; RAF PROTEIN; RESORCINOL; TRIAZOLE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; VER 49009;

ANTINEOPLASTIC ACTIVITY; CANCER CELL; CANCER CELL CULTURE; CANCER INHIBITION; CANCER THERAPY; CELL PROLIFERATION; CLINICAL TRIAL; COMPLEX FORMATION; DRUG MECHANISM; DRUG RESEARCH; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; IC 50; IN VIVO STUDY; MALIGNANT NEOPLASTIC DISEASE; NONHUMAN; PROTEIN DOMAIN; PROTEIN FUNCTION; PROTEIN TARGETING; REVIEW; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; TUMOR GROWTH; TUMOR XENOGRAFT; X RAY CRYSTALLOGRAPHY;

ANIMALS; ANTINEOPLASTIC AGENTS; DRUG DESIGN; HSP90 HEAT-SHOCK PROTEINS; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NEOPLASMS; PYRAZOLES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 33746341544     PISSN: 15680266     EISSN: None     Source Type: Journal    
DOI: 10.2174/156802606777812086     Document Type: Review

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