The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 5, 2010, Pages 1491-1495

  Schiemann, Kai ^a   Finsinger, Dirk ^a   Zenke, Frank ^a   Amendt, Christiane ^a   Knöchel, Thorsten ^a   Bruge, David ^a   Buchstaller, Hans Peter ^a   Emde, Ulrich ^a   Stähle, Wolfgang ^a   Anzali, Soheila ^b  

^a Merck Serono GmbH   (Germany)

^b MERCK KGAA   (Germany)

Author keywords

Anti mitotic agents; Eg5 inhibitors; EMD 534085; Kinesin spindle protein; Kinesin 5; KSP; SAR

Indexed keywords

ADENOSINE TRIPHOSPHATASE INHIBITOR; ANTIMITOTIC AGENT; ANTINEOPLASTIC AGENT; EMD 534085; HEXAHYDRO 2H PYRANO[3,2 C]QUINOLINE DERIVATIVE; KINESIN; KINESIN 5; NUCLEOTIDE; QUINOLINE DERIVATIVE; UNCLASSIFIED DRUG;

ALLOSTERISM; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; APOPTOSIS; ARTICLE; BINDING SITE; CANCER INHIBITION; CARCINOMA CELL; CELL ACTIVITY; CELL CYCLE ARREST; COLON CARCINOMA; CONTROLLED STUDY; DOSE RESPONSE; DRUG DOSE COMPARISON; DRUG POTENCY; DRUG SELECTIVITY; ENZYME ACTIVITY; ENZYME INHIBITION; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; LOW DRUG DOSE; MICROTUBULE; MITOSIS INHIBITION; MOUSE; NONHUMAN; WEIGHT REDUCTION; X RAY CRYSTALLOGRAPHY;

ALLOSTERIC REGULATION; ANIMALS; ANTINEOPLASTIC AGENTS; BINDING SITES; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; DRUG DISCOVERY; ENZYME INHIBITORS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; KINESIN; MICE; MITOSIS; QUINOLINES; STRUCTURE-ACTIVITY RELATIONSHIP; XENOGRAFT MODEL ANTITUMOR ASSAYS;

CITRUS MACROPHYLLA;

EID: 76749108514     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.01.110     Document Type: Article

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