Publications [#233150] of Dewey G. McCafferty

Journal Articles

  1. Kapustin, GV; Fejér, G; Gronlund, JL; McCafferty, DG; Seto, E; Etzkorn, FA, "Phosphorus-based SAHA analogues as histone deacetylase inhibitors.", Organic lettersAugust,, 2003, 5(17), 3053-3056 [doi].
    (last updated on 2024/07/16)

    Abstract:
    [structure: see text] Three analogues of suberoyl anilide hydroxamic acid (SAHA) with phosphorus metal-chelating functionalities were synthesized as inhibitors of histone deacetylases (HDACs). The compounds showed weak activity for HeLa nuclear extracts (IC(50) = 0.57-6.1 mM), HDAC8 (IC(50) = 0.28-0.41 mM), and histone-deacetylase-like protein (HDLP, IC(50) = 0.33-1.9 mM), suggesting that the transition state of HDAC is not analogous to zinc proteases. Antiproliferative activity against A2780 cancer cells (IC(50) = 0.11-0.12 mM), comparable to SAHA (0.15 mM), was observed.