Bioorganic and Medicinal Chemistry Letters p. 283 - 287 (2004)
Update date:2022-08-05
Topics:
Vaisburg, Arkadii
Bernstein, Naomy
Frechette, Sylvie
Allan, Martin
Abou-Khalil, Elie
Leit, Silvana
Moradei, Oscar
Bouchain, Giliane
Wang, James
Woo, Soon Hyung
Fournel, Marielle
Yan, Pu T.
Trachy-Bourget, Marie-Claude
Kalita, Ann
Beaulieu, Carole
Li, Zuomei
MacLeod, A. Robert
Besterman, Jeffrey M.
Delorme, Daniel
A variety of ω-substituted alkanoic acid (2-amino-phenyl)-amides were designed and synthesized. These compounds were shown to inhibit recombinant human histone deacetylases (HDACs) with IC50 values in the low micromolar range and induce hyperacetylation of histones in whole cells. They induced expression of p21WAF1/Cip1 and caused cell-cycle arrest in human cancer cells. Compounds in this class showed efficacy in human tumor xenograft models.
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