Title of article
Synthesis of pyrazoles and isoxazoles as potent αvβ3 receptor antagonists
Author/Authors
Thomas D. Penning، نويسنده , , Albert Khilevich، نويسنده , , Barbara B. Chen، نويسنده , , Mark A. Russell، نويسنده , , Mark L. Boys، نويسنده , , Yaping Wang، نويسنده , , Tiffany Duffin، نويسنده , , V. Wayne Engleman، نويسنده , , Mary Beth Finn، نويسنده , , Sandra K. Freeman، نويسنده , , Melanie L. Hanneke، نويسنده , , Jeffery L. Keene، نويسنده , , Jon A. Klover، نويسنده , , G. Allen Nickols، نويسنده , , Maureen A. Nickols، نويسنده , , Randall K. Rader، نويسنده , , Steven L. Settle، نويسنده , , Kristen E. Shannon، نويسنده , , Christina N. Steininger، نويسنده , , Marisa M. Westlin، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
6
From page
3156
To page
3161
Abstract
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. In HT29 cells, most analogs also demonstrated significant selectivity against αvβ6. Several compounds showed good pharmacokinetic properties in rats, in addition to anti-angiogenic activity in a mouse corneal micropocket model. Compounds were synthesized in a straightforward manner from readily available glutarate precursors.
Keywords
Integrin antagonist , ?v?3 , RGD peptidomimetic
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796946
Link To Document