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1.
Bioorg Med Chem Lett ; 16(4): 839-44, 2006 Feb 15.
Article in English | MEDLINE | ID: mdl-16298127

ABSTRACT

We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin alpha(v)beta3 and, in addition, show selectivity relative to the other beta3 integrin alpha(IIb)beta3. In whole cells, the majority of these analogs also demonstrated modest selectivity against other alpha(v) integrins such as alpha(v)beta1 and alpha(v)beta6.


Subject(s)
Butyrates/chemical synthesis , Butyrates/pharmacology , Integrin alphaVbeta3/antagonists & inhibitors , Oxadiazoles/chemical synthesis , Oxadiazoles/pharmacology , Antigens, Neoplasm , Butyrates/chemistry , Cell Line , Humans , Integrins/antagonists & inhibitors , Molecular Structure , Oxadiazoles/chemistry , Receptors, Vitronectin/antagonists & inhibitors , Structure-Activity Relationship
2.
Bioorg Med Chem Lett ; 15(1): 93-8, 2005 Jan 03.
Article in English | MEDLINE | ID: mdl-15582418

ABSTRACT

A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors.


Subject(s)
Naphthalenes/pharmacokinetics , Plasminogen Inactivators/pharmacokinetics , Urokinase-Type Plasminogen Activator/antagonists & inhibitors , Models, Molecular , Naphthalenes/chemistry , Plasminogen Inactivators/chemistry , Substrate Specificity
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