Jh. Tatlock et al., HIGH-AFFINITY FKBP-12 LIGANDS DERIVED FROM (R)-(-)-CARVONE - SYNTHESIS AND EVALUATION OF PK506 PYRANOSE RING REPLACEMENTS, Bioorganic & medicinal chemistry letters, 5(21), 1995, pp. 2489-2494
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 syn
thetically more accessible. The versatility of these FKBP-12 ligands i
s demonstrated with respect to effector domain exploration.