4759-64-2Relevant academic research and scientific papers
Synthesis of 2,5-thiazole butanoic acids as potent and selective αvβ3 integrin receptor antagonists with improved oral pharmacokinetic properties
Wendt, John A.,Wu, Hongwei,Stenmark, Heather G.,Boys, Mark L.,Downs, Victoria L.,Penning, Thomas D.,Chen, Barbara B.,Wang, Yaping,Duffin, Tiffany,Finn, Mary Beth,Keene, Jeffery L.,Engleman, V. Wayne,Freeman, Sandra K.,Hanneke, Melanie L.,Shannon, Kristen E.,Nickols, Maureen A.,Steininger, Christina N.,Westlin, Marissa,Klover, Jon A.,Westlin, William,Nickols, G. Allen,Russell, Mark A.
, p. 845 - 849 (2007/10/03)
We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin αvβ3 and show selectivity relative to the other integrins, such as αIIbβ 3 and αvβ6. These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs.
Synthesis of pyrazoles and isoxazoles as potent αvβ3 receptor antagonists
Penning, Thomas D.,Khilevich, Albert,Chen, Barbara B.,Russell, Mark A.,Boys, Mark L.,Wang, Yaping,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.,Rader, Randall K.,Settle, Steven L.,Shannon, Kristen E.,Steininger, Christina N.,Westlin, Marisa M.,Westlin, William F.
, p. 3156 - 3161 (2007/10/03)
We describe a series of pyrazole and isoxazole analogs as antagonists of the αvβ3 receptor. Compounds showed low to sub-nanomolar potency against αvβ3, as well as good selectivity against αIIbβ3
