14689-51-1Relevant articles and documents
Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1
Llona-Minguez, Sabin,H?glund, Andreas,Jacques, Sylvain A.,Johansson, Lars,Calderón-Monta?o, José Manuel,Claesson, Magnus,Loseva, Olga,Valerie, Nicholas C. K.,Lundb?ck, Thomas,Piedrafita, Javier,Maga, Giovanni,Crespan, Emmanuele,Meijer, Laurent,Burgos Morón, Estefanía,Baranczewski, Pawel,Hagbj?rk, Ann-Louise,Svensson, Richard,Wiita, Elisee,Alml?f, Ingrid,Visnes, Torkild,Jeppsson, Fredrik,Sigmundsson, Kristmundur,Jensen, Annika Jenmalm,Artursson, Per,Jemth, Ann-Sofie,Stenmark, P?l,Warpman Berglund, Ulrika,Scobie, Martin,Helleday, Thomas
, p. 1140 - 1148 (2016)
The dCTPase pyrophosphatase 1 (dCTPase) regulates the intracellular nucleotide pool through hydrolytic degradation of canonical and noncanonical nucleotide triphosphates (dNTPs). dCTPase is highly expressed in multiple carcinomas and is associated with cancer cell stemness. Here we report on the development of the first potent and selective dCTPase inhibitors that enhance the cytotoxic effect of cytidine analogues in leukemia cells. Boronate 30 displays a promising in vitro ADME profile, including plasma and mouse microsomal half-lives, aqueous solubility, cell permeability and CYP inhibition, deeming it a suitable compound for in vivo studies.
New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phneylpiperazine dopaminergic template
Mewshaw, Richard E.,Verwijs, Antoine,Shi, Xiaojie,McGaughey, Georgia B.,Nelson, James A.,Mazandarani, Hossein,Brennan, Julie A.,Marquis, Karen L.,Coupet, Joseph,Andree, Terrance H.
, p. 2675 - 2680 (2007/10/03)
The synthesis of several bioisoteric analogs based on the 3-OH-N1- phenylpiperazine dopamine D2 agonist template (i.e., 4) is described. The indolone (5) and 2-CF3-benzimidazole (13) were observed to have excellent affinity for the D2 receptor. Several D4 selective compounds were also identified. Molecular modeling studies and a putative bioactive conformation are discussed.
