23938-71-8Relevant articles and documents
NOVEL SUBSTITUTED CONDENSED PYRIMIDINE COMPOUNDS
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Page/Page column 36, (2015/02/25)
Novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.
Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors
Thomas, Allen A.,Le Huerou,De Meese,Gunawardana, Indrani,Kaplan, Tomas,Romoff, Todd T.,Gonzales, Stephen S.,Condroski, Kevin,Boyd, Steven A.,Ballard, Josh,Bernat, Bryan,DeWolf, Walter,Han, May,Lee, Patrice,Lemieux, Christine,Pedersen, Robin,Pheneger, Jed,Poch, Greg,Smith, Darin,Sullivan, Francis,Weiler, Solly,Wright, S. Kirk,Lin, Jie,Brandhuber, Barb,Vigers, Guy
, p. 2206 - 2210 (2008/12/20)
Tumor cells extensively utilize the pentose phosphate pathway for the synthesis of ribose. Transketolase is a key enzyme in this pathway and has been suggested as a target for inhibition in the treatment of cancer. In a pharmacodynamic study, nude mice with xenografted HCT-116 tumors were dosed with 1 ('N3′-pyridyl thiamine'; 3-(6-methyl-2-amino-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazol-3-ium chloride hydrochloride), an analog of thiamine, the co-factor of transketolase. Transketolase activity was almost completely suppressed in blood, spleen, and tumor cells, but there was little effect on the activity of the other thiamine-utilizing enzymes α-ketoglutarate dehydrogenase or glucose-6-phosphate dehydrogenase. Synthesis and SAR of transketolase inhibitors is described.
Synthesis and biological activity substituted of 2-(4-imidazolyl)ethylamines
Plazzi,Bordi,Vitto,Impicciatore
, p. 921 - 931 (2007/10/02)
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