Sulfamides as novel histone deacetylase inhibitors.

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Wahhab A, Smil D, Ajamian A, Allan M, Chantigny Y, Therrien E, Nguyen N, Manku S, Leit S, Rahil J, Petschner AJ, Lu AH, Nicolescu A, Lefebvre S, Montcalm S, Fournel M, Yan TP, Li Z, Besterman JM, Deziel R

Sulfamides as novel histone deacetylase inhibitors.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):336-40. doi: 10.1016/j.bmcl.2008.11.081. Epub 2008 Nov 27.

PubMed ID
19084395 [ View in PubMed
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Abstract

The sulfamide moiety has been utilized to design novel HDAC inhibitors. The potency and selectivity of these inhibitors were influenced both by the nature of the scaffold, and the capping group. Linear long-chain-based analogs were primarily HDAC6-selective, while analogs based on the lysine scaffold resulted in potent HDAC1 and HDAC6 inhibitors.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
VorinostatHistone deacetylase 1IC 50 (nM)100N/AN/ADetails
VorinostatHistone deacetylase 1IC 50 (nM)600N/AN/ADetails
VorinostatHistone deacetylase 6IC 50 (nM)200N/AN/ADetails