Kinesin spindle protein (KSP) inhibitors. Part 3: Synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 7, 2006, Pages 1780-1783

  Garbaccio, Robert M ^a   Fraley, Mark E ^a   Tasber, Edward S ^a   Olson, Christy M ^a   Hoffman, William F ^a   Arrington, Kenneth L ^a   Torrent, Maricel ^a   Buser, Carolyn A ^a   Walsh, Eileen S ^a   Hamilton, Kelly ^a   Schaber, Michael D ^a   Fernandes, Christine ^a   Lobell, Robert B ^a   Tao, Weikang ^a   South, Vicki J ^a   Yan, Youwei ^a   Kuo, Lawrence C ^a   Prueksaritanont, Thomayant ^a   Slaughter, Donald E ^a   Shu, Cathy ^a   Heimbrook, David C ^a   Kohl, Nancy E ^a   Huber, Hans E ^a   Hartman, George D ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Antimitotic; Cancer; Dihydropyrrole; hERG; Kinesin; Kinesin spindle protein; KSP; Phenol; Phosphate prodrug

Indexed keywords

ANTIMITOTIC AGENT; KINESIN SPINDLE PROTEIN INHIBITOR; PHENOL DERIVATIVE; PHOSPHATE; POTASSIUM CHANNEL HERG; PRODRUG; PROTEIN INHIBITOR; PYRROLE DERIVATIVE; UNCLASSIFIED DRUG;

AQUEOUS SOLUTION; AREA UNDER THE CURVE; ARTICLE; CANCER THERAPY; CHIRAL CHROMATOGRAPHY; DRUG DESIGN; DRUG SYNTHESIS; PURIFICATION; REDUCTION; X RAY CRYSTALLOGRAPHY;

ANIMALS; AREA UNDER CURVE; DOGS; ETHER-A-GO-GO POTASSIUM CHANNELS; KINESIN; MITOTIC SPINDLE APPARATUS; PRODRUGS; PROTEIN BINDING; PYRROLES; RATS; SOLUBILITY; WATER;

EID: 33144455399     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.12.094     Document Type: Article

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