1007556-16-2Relevant academic research and scientific papers
Synthesis and pharmacophore modelling of 2,6,9-trisubstituted purine derivatives and their potential role as apoptosis-inducing agents in cancer cell lines
Calderón-Arancibia, Jeannette,Espinosa-Bustos, Christian,Ca?ete-Molina, álvaro,Tapia, Ricardo A.,Faúndez, Mario,Torres, Maria Jose,Aguirre, Adam,Paulino, Margot,Salas, Cristian O.
, p. 6808 - 6826 (2015)
Twelve compounds were obtained by a three step synthetic procedure using microwave irradiation in a pivotal step. All compounds were evaluated in vitro to determine their potential effect on cell toxicity by the MTT method and flow cytometry analysis on four cancer cells lines and Vero cells. Three out of twelve compounds were found to be promising agents compared to a known and effective anticancer drug, etoposide, in three out of four cancer cell lines assayed with considerable selectivity. Preliminary flow cytometry data suggests that compounds mentioned above induce apoptosis on these cells. The main structural requirements for their activity for each cancer cell line were characterized with a preliminary pharmacophore model, which identified aromatic centers, hydrogen acceptor/donor center and a hydrophobic area. These features were consistent with the cytotoxic activity of the assayed compounds.
Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB
Mallari, Jeremy P.,Shelat, Anang A.,Obrien, Terri,Caffrey, Conor R.,Kosinski, Aaron,Connelly, Michele,Harbut, Michael,Greenbaum, Doron,McKerrow, James H.,Guy, R. Kiplin
, p. 545 - 552 (2008/09/18)
Human African trypanosomiasis (HAT), a major health concern in sub-Saharan Africa, is caused by the protozoan parasite Trypanosoma brucei. Recent studies have shown that a cathepsin B like protease, TbcatB, is essential to the survival of T. brucei in vit
