873225-52-6Relevant academic research and scientific papers
SNAr reactions of 2-methylthio-4-pyrimidinones in pivalic acid: Access to functionalized pyrimidinones and pyrimidines
Maddess, Matthew L.,Carter, Rhiannon
experimental part, p. 1109 - 1118 (2012/05/04)
Pivalic acid is a useful medium to effect the direct SNAr displacement of 2-methylthio-4-pyrimidinones with a variety of anilines. Products are easily isolated in good to excellent yields, and following chlorination, provide an opportunity to r
Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK
Waelchli, Rudolf,Bollbuck, Birgit,Bruns, Christian,Buhl, Thomas,Eder, Joerg,Feifel, Roland,Hersperger, Rene,Janser, Philipp,Revesz, Laszlo,Zerwes, Hans-Guenter,Schlapbach, Achim
, p. 108 - 112 (2007/10/03)
The design, synthesis, and the biological evaluation of 2-benzamido-pyrimidines as novel IKK inhibitors are described. By optimization of the lead compound 3, compounds 16 and 24 are identified as good inhibitors of IKK2 with IC50 values of 40 and 25 nM, respectively. Compound 16 also demonstrated significant in vivo activity in an acute model of cytokine release.
