High-affinity FKBP-12 ligands derived from (R)-(−)-carvone. Synthesis and evaluation of FK506 pyranose ring replacements

Autor: J. V. French, Richard E. Showalter, Hans E. Parge, Vincent J. Kalish, Daniel R. Knighton, John H. Tatlock, Christina T. Lewis, J. Ernest Villafranca
Rok vydání: 1995
Předmět:
Zdroj: Bioorganic & Medicinal Chemistry Letters. 5:2489-2494
ISSN: 0960-894X
DOI: 10.1016/0960-894x(95)00429-w
Popis: The preparation and evaluation of potent small molecule inhibitors of FKBP-12 rotamase activity is described. These ligands contain many of the structural features of the FK506 pyranose ring region, yet are synthetically more accessible. The versatility of these FKBP-12 ligands is demonstrated with respect to effector domain exploration.
Databáze: OpenAIRE