Journal of Medicinal Chemistry p. 1772 - 1776 (2013)
Update date:2022-08-04
Topics:
Wagner, Florence F.
Olson, David E.
Gale, Jennifer P.
Kaya, Taner
We?wer, Michel
Aidoud, Nadia
Thomas, Méryl
Davoine, Emeline L.
Lemercier, Bérénice C.
Zhang, Yan-Ling
Holson, Edward B.
Hydroxamic acids were designed, synthesized, and evaluated for their ability to selectively inhibit human histone deacetylase 6 (HDAC6). Several inhibitors, including compound 14 (BRD9757), exhibited excellent potency and selectivity despite the absence of a surface-binding motif. The binding of these highly efficient ligands for HDAC6 is rationalized via structure-activity relationships. These results demonstrate that high selectivity and potent inhibition of HDAC6 can be achieved through careful choice of linker element only.
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