Highly Ligand Efficient and SelectiveN-2-(Thioethyl)picolinamide Histone Deacetylase Inhibitors Inspired by the Natural Product Psammaplin A

ChemMedChem ◽  
2012 ◽  
Vol 8 (1) ◽  
pp. 149-156 ◽  
Author(s):  
Matthias G. J. Baud ◽  
Patricia Haus ◽  
Thomas Leiser ◽  
Franz-Josef Meyer-Almes ◽  
Matthew J. Fuchter
Keyword(s):  
Natural Product ◽  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Psammaplin A

scholarly journals Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors

2013 ◽  
Vol 9 ◽  
pp. 81-88 ◽  
Author(s):  
Matthias G J Baud ◽  
Thomas Leiser ◽  
Vanessa Petrucci ◽  
Mekala Gunaratnam ◽  
Stephen Neidle ◽  
...  
Keyword(s):  
Natural Product ◽  
Histone Deacetylase ◽  
Mechanism Of Action ◽  
Inhibitory Activity ◽  
Histone Deacetylase Inhibitors ◽  
Hdac Inhibitors ◽  
Psammaplin A ◽  
Significant Interest ◽  
Thiol Form ◽  
Derivatives Of

There has been significant interest in the bioactivity of the natural product psammaplin A, most recently as a potent and isoform selective HDAC inhibitor. Here we report our preliminary studies on thioester HDAC inhibitors derived from the active monomeric (thiol) form of psammaplin A, as a means to improve compound delivery into cells. We have discovered that such compounds exhibit both potent cytotoxicity and enzymatic inhibitory activity against recombinant HDAC1. The latter effect is surprising since previous SAR suggested that modification of the thiol functionality should detrimentally affect HDAC potency. We therefore also report our preliminary studies on the mechanism of action of this observed effect.

Natural Product-based Screening for Histone Deacetylase Inhibitors

Planta Medica ◽  
2007 ◽  
Vol 73 (09) ◽  
Author(s):  
S Krasteva ◽  
EH Heiss ◽  
V Dirsch ◽  
L Krenn
Keyword(s):  
Natural Product ◽  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors
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