| Autor: |
Duggan, M. E., Duong, L. T., Fisher, J. E., Hamill, T. G., Hoffman, W. F., Huff, J. R., Ihle, N. C., Leu, C.-T., Nagy, R. M., Perkins, J. J., Rodan, S. B., Wesolowski, G., Whitman, D. B., Zartman, A. E., Rodan, G. A., Hartman, G. D. |
| Zdroj: |
Journal of Medicinal Chemistry; October 5, 2000, Vol. 43 Issue: 20 p3736-3745, 10p |
| Abstrakt: |
Modification of the potent fibrinogen receptor (αIIbβ3) antagonist 1 generated compounds with high affinity for the vitronectin receptor αvβ3. Sequential modification of the basic N-terminus of 1 led to the identification of the 5,6,7,8-tetrahydro[1,8]naphthyridine moiety (THN) as a lipophilic, moderately basic N-terminus that provides molecules with excellent potency and selectivity for the integrin receptor αvβ3. The THN-containing analogue 5 is a potent inhibitor of bone resorption in vitro and in vivo. In addition, the identification of a novel, nonpeptide radioligand with high affinity to αvβ3 is also reported. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
|
