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1.
Bioorg Med Chem Lett ; 18(20): 5487-92, 2008 Oct 15.
Article in English | MEDLINE | ID: mdl-18815031

ABSTRACT

An imidazole series of cyclin-dependent kinase (CDK) inhibitors has been developed. Protein inhibitor structure determination has provided an understanding of the emerging structure activity trends for the imidazole series. The introduction of a methyl sulfone at the aniline terminus led to a more orally bioavailable CDK inhibitor that was progressed into clinical development.


Subject(s)
Cyclin-Dependent Kinases/antagonists & inhibitors , Imidazoles/chemistry , Aniline Compounds/chemistry , Animals , Cell Cycle Proteins/chemistry , Chemistry, Pharmaceutical/methods , Crystallography, X-Ray/methods , Drug Design , Humans , Hydrogen Bonding , Inhibitory Concentration 50 , Mice , Models, Chemical , Molecular Conformation , Structure-Activity Relationship
2.
Bioorg Med Chem Lett ; 14(2): 405-8, 2004 Jan 19.
Article in English | MEDLINE | ID: mdl-14698169

ABSTRACT

Screening of the corporate database led to the discovery of a novel series of N-benzylindole-2-carboxylic acid CCR2b chemokine receptor antagonists. These compounds demonstrate high affinity and functional inhibition of the CCR2b receptor. A discussion of the structure-activity relationships is presented, together with evidence for a highly selective receptor binding profile.


Subject(s)
Benzyl Compounds/pharmacology , Carboxylic Acids/pharmacology , Indoles/pharmacology , Receptors, Chemokine/antagonists & inhibitors , Receptors, Chemokine/metabolism , Benzyl Compounds/metabolism , Carboxylic Acids/metabolism , Indoles/metabolism , Protein Binding/physiology , Receptors, CCR2
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