78648-41-6Relevant articles and documents
Cytidine deaminase can deaminate fused pyrimidine ribonucleosides
Li, Yao,Ludford, Paul T.,Tor, Yitzhak,Yang, Shenghua
supporting information, p. 6237 - 6243 (2021/07/28)
The tolerance of cytidine deaminase (CDA) to expanded heterocycles is exploredviathree fluorescent cytidine analogues, where the pyrimidine core is fused to three distinct five-membered heterocycles at the 5/6 positions. The reaction between CDA and each analogue is followed by absorption and emission spectroscopy, revealing shorter reaction times for all analogues than the native substrate. Pseudo-first order and Michaelis-Menten kinetic analyses provide insight into the enzymatic deamination reactions and assist in drawing comparison to established structure activity relationships. Finally, inhibitor screening modalities are created for each analogue and validated with zebularine and tetrahydrouridine, two known CDA inhibitors.
Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors
Bencsik, Josef R.,Xiao, Dengming,Blake, James F.,Kallan, Nicholas C.,Mitchell, Ian S.,Spencer, Keith L.,Xu, Rui,Gloor, Susan L.,Martinson, Matthew,Risom, Tyler,Woessner, Richard D.,Dizon, Faith,Wu, Wen-I,Vigers, Guy P.A.,Brandhuber, Barbara J.,Skelton, Nicholas J.,Prior, Wei Wei,Murray, Lesley J.
scheme or table, p. 7037 - 7041 (2010/12/25)
Herein we report the discovery and synthesis of a novel series of dihydrothieno- and dihydrofuropyrimidines (2 and 3) as potent pan Akt inhibitors. Utilizing previous SAR and analysis of the amino acid sequences in the binding site we have designed inhibi
2-Phenyl-5,6-dihydro-2H-thieno[3,2-c]pyrazol-3-ol derivatives as new inhibitors of bacterial cell wall biosynthesis
Li, Zhong,Francisco, Gerardo D.,Hu, William,Labthavikul, Pornpen,Petersen, Peter J.,Severin, Anatoly,Singh, Guy,Yang, Youjun,Rasmussen, Beth A.,Lin, Yang-I,Skotnicki, Jerauld S.,Mansour, Tarek S.
, p. 2591 - 2594 (2007/10/03)
Twenty-five 2-phenyl-5,6-dihydro-2H-thieno[3,2-c]pyrazol-3-ol derivatives were synthesized for evaluation as new inhibitors of bacterial cell wall biosynthesis. Many of them demonstrated good inhibitory activity against Staphylococcus aureus MurB, MurC and MurD enzymes in vitro and antimicrobial activity against gram-positive bacteria including MRSA, VRE and PRSP. However, when they were tested in the presence of 4% bovine serum albumin, the MIC values increased to greater than 128 μg/mL against PRSP. None of the compounds demonstrated activity against gram-negative bacteria at MIC 32 μg/mL.
