Convergent, parallel synthesis of a series of beta-substituted 1,2,4-oxadiazole butanoic acids as potent and selective alpha(v)beta3 receptor antagonists

Convergent, parallel synthesis of a series of beta-substituted 1,2,4-oxadiazole butanoic acids as potent and selective alpha(v)beta3 receptor antagonists

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) int...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-02, Vol.16 (4), p.839-844
Hauptverfasser: Boys, Mark L, Schretzman, Lori A, Chandrakumar, Nizal S, Tollefson, Michael B, Mohler, Scott B, Downs, Victoria L, Penning, Thomas D, Russell, Mark A, Wendt, John A, Chen, Barbara B, Stenmark, Heather G, Wu, Hongwei, Spangler, Dale P, Clare, Michael, Desai, Bipin N, Khanna, Ish K, Nguyen, Maria N, Duffin, Tiffany, Engleman, V Wayne, Finn, Mary Beth, Freeman, Sandra K, Hanneke, Melanie L, Keene, Jeffery L, Klover, Jon A, Nickols, G Allen, Nickols, Maureen A, Steininger, Christina N, Westlin, Marisa, Westlin, William, Yu, Yi X, Wang, Yaping, Dalton, Christopher R, Norring, Sarah A
Format: Artikel
Sprache:eng
Schlagworte:
Antigens, Neoplasm
Butyrates - chemical synthesis
Butyrates - chemistry
Butyrates - pharmacology
Cell Line
Humans
Integrin alphaVbeta3 - antagonists & inhibitors
Integrins - antagonists & inhibitors
Molecular Structure
Oxadiazoles - chemical synthesis
Oxadiazoles - chemistry
Oxadiazoles - pharmacology
Receptors, Vitronectin - antagonists & inhibitors
Structure-Activity Relationship
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Zusammenfassung: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.
ISSN:0960-894X