Discovery and structure-activity relationships of novel piperidine inhibitors of farnesyltransferase

Journal of Medicinal Chemistry

Volumn 46, Issue 12, 2003, Pages 2467-2473

  Nara, Shinji ^a   Tanaka, Rieko ^a   Eishima, Jun ^a   Hara, Mitsunobu ^a   Takahashi, Yuichi ^a   Otaki, Shizuo ^a   Foglesong, Robert J ^b   Hughes, Philip F ^b   Turkington, Shelley ^b   Kanda, Yutaka ^a  

^a KYOWA HAKKO KOGYO CO LTD   (Japan)

^b ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 BENZYL 7 CYANO 2,3,4,5 TETRAHYDRO 1 (1H IMIDAZOL 4 YLMETHYL) 4 (2 THIENYLSULFONYL) 1H 1,4 BENZODIAZEPINE; 4 (2 BROMOPHENYL) 2 (3,4 DIHYDROXYPHENYL) 3 NITRO 1 (3 PYRIDYLMETHYL)PIPERIDINE; ANTINEOPLASTIC AGENT; LEAD; LONAFARNIB; PIPERIDINE DERIVATIVE; PROTEIN FARNESYLTRANSFERASE INHIBITOR; RAS PROTEIN; TIPIFARNIB; UNCLASSIFIED DRUG;

ARTICLE; CHIRALITY; DRUG ACTIVITY; DRUG POTENCY; DRUG SYNTHESIS; ENANTIOMER; OPTICAL ROTATION; STRUCTURE ACTIVITY RELATION;

ALKYL AND ARYL TRANSFERASES; ANIMALS; CATTLE; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; COMBINATORIAL CHEMISTRY TECHNIQUES; CRYSTALLOGRAPHY, X-RAY; ENZYME INHIBITORS; FARNESYLTRANSTRANSFERASE; HUMANS; KINETICS; MAGNETIC RESONANCE SPECTROSCOPY; PIPERIDINES; RAS PROTEINS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TUMOR CELLS, CULTURED;

EID: 12444334604     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm020522k     Document Type: Article

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15. 50 of 39 nM. Detailed results of cellular assays as well as biochemical studies of this class of compounds will be described elsewhere. Hara, M.; et al. Manuscript in preparation.