3-Aminopyrrolidinone farnesyltransferase inhibitors: Design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency

Journal of Medicinal Chemistry

Volumn 45, Issue 12, 2002, Pages 2388-2409

  Bell, Ian M ^a   Gallicchio, Steven N ^a   Abrams, Marc ^a   Beese, Lorena S ^b   Beshore, Douglas C ^a   Bhimnathwala, Hema ^a   Bogusky, Michael J ^a   Buser, Carolyn A ^a   Culberson, J Christopher ^a   Davide, Joseph ^a   Ellis Hutchings, Michelle ^a   Fernandes, Christine ^a   Gibbs, Jackson B ^a   Graham, Samuel L ^a   Hamilton, Kelly A ^a   Hartman, George D ^a   Heimbrook, David C ^a   Homnick, Carl F ^a   Huber, Hans E ^a   Huff, Joel R ^a   Kassahun, Kelem ^a   Koblan, Kenneth S ^a   Kohl, Nancy E ^a   Lobell, Robert B ^a   Lynch Jr , Joseph J ^a   Robinson, Ronald ^a   Rodrigues, A David ^a   Taylor, Jeffrey S ^b   Walsh, Eileen S ^a   Williams, Theresa M ^a   Zartmant, C Blair ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

^b DUKE UNIVERSITY MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

MACROCYCLIC COMPOUND; PROTEIN FARNESYLTRANSFERASE INHIBITOR; PYRROLIDINE DERIVATIVE;

ARTICLE; BIOAVAILABILITY; CHEMICAL ANALYSIS; CRYSTAL STRUCTURE; DOG; ENZYME INHIBITION; ENZYME SYNTHESIS; LIVER MICROSOME; NONHUMAN; ONCOGENE RAS; PLASMA HALF LIFE; X RAY CRYSTALLOGRAPHY;

ALKYL AND ARYL TRANSFERASES; ANIMALS; ARYL HYDROCARBON HYDROXYLASES; CATION TRANSPORT PROTEINS; CELL LINE; CHROMATOGRAPHY, LIQUID; CRYSTALLOGRAPHY, X-RAY; CYTOCHROME P-450 CYP3A; CYTOCHROME P-450 ENZYME SYSTEM; DNA-BINDING PROTEINS; DOGS; ELECTROCARDIOGRAPHY; ENZYME INHIBITORS; ETHER-A-GO-GO POTASSIUM CHANNELS; FARNESYLTRANSTRANSFERASE; HUMANS; MAGNETIC RESONANCE SPECTROSCOPY; MASS SPECTROMETRY; MICROSOMES, LIVER; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NAPHTHALENES; OXIDOREDUCTASES, N-DEMETHYLATING; POTASSIUM CHANNELS; POTASSIUM CHANNELS, VOLTAGE-GATED; PROTEIN BINDING; PYRROLIDINES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TRANS-ACTIVATORS;

EID: 0037030606     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm010531d     Document Type: Article

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