645401-60-1Relevant academic research and scientific papers
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
Paquin, Isabelle,Raeppel, Stephane,Leit, Silvana,Gaudette, Frederic,Zhou, Nancy,Moradei, Oscar,Saavedra, Oscar,Bernstein, Naomy,Raeppel, Franck,Bouchain, Giliane,Frechette, Sylvie,Woo, Soon H.,Vaisburg, Arkadii,Fournel, Marielle,Kalita, Ann,Robert, Marie-France,Lu, Aihua,Trachy-Bourget, Marie-Claude,Yan, Pu Theresa,Liu, Jianhong,Rahil, Jubrail,MacLeod, A. Robert,Besterman, Jeffrey M.,Li, Zuomei,Delorme, Daniel
, p. 1067 - 1071 (2008/09/18)
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
2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: Highly potent, orally active, adenosine A2A antagonists. Part 1
Matasi, Julius J.,Caldwell, John P.,Zhang, Hongtao,Fawzi, Ahmad,Cohen-Williams, Mary E.,Varty, Geoffrey B.,Tulshian, Deen B.
, p. 3670 - 3674 (2007/10/03)
The structure-activity relationship of this novel class of compounds based on 2-(2-furanyl)-7-phenyl[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, 1, and its analogs was evaluated for their in vitro and in vivo adenosine A2A receptor antagonism. Several compounds displayed oral activity at 3 mg/kg in a rat catalepsy model. Specifically, compound 8g displayed an excellent in vitro profile, as well as a highly promising in vivo profile.
