Title of article :
Design and synthesis of 4-[(s-triazin-2-ylamino)methyl]-N-(2-aminophenyl)-benzamides and their analogues as a novel class of histone deacetylase inhibitors
Author/Authors :
Isabelle Paquin، نويسنده , , Stéphane Raeppel، نويسنده , , Silvana Leit، نويسنده , , Frédéric Gaudette، نويسنده , , Nancy Zhou، نويسنده , , Oscar Moradei، نويسنده , , Oscar Saavedra، نويسنده , , Naomy Bernstein، نويسنده , , Franck Raeppel، نويسنده , , Giliane Bouchain، نويسنده , , Sylvie Frechette، نويسنده , , Soon H. Woo، نويسنده , , Arkadii Vaisburg، نويسنده , , Marielle Fournel، نويسنده , , Ann Kalita، نويسنده , , Marie-France Robert، نويسنده , , Aihua Lü، نويسنده , , Marie-Claude Trachy-Bourget، نويسنده , , Pu Theresa Yan، نويسنده , , Jianhong Liu، نويسنده , , et al.، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Pages :
5
From page :
1067
To page :
1071
Abstract :
Inhibition of histone deacetylases (HDAC) is emerging as a new strategy in human cancer therapy. The synthesis and biological evaluation of a variety of 4-(heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides is presented herein. From the different series bearing a six-membered heteroaromatic ring studied, the s-triazine series showed the best HDAC1 enzyme and in vitro anti-proliferative activities with IC50 values below micromolar range. Some of these compounds can also significantly reduce tumor growth in human tumor xenograft models in mice.
Keywords :
Histone deacetylases (HDACs) , HDAC inhibitor , Anti-proliferative activity , s-Triazine , benzamides
Journal title :
Bioorganic & Medicinal Chemistry Letters
Serial Year :
2008
Journal title :
Bioorganic & Medicinal Chemistry Letters
Record number :
799115
Link To Document :
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