24248-71-3Relevant academic research and scientific papers
Parallel synthesis and biological evaluation of 5,6,7,8- tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-one cytotoxic agents selective for p21-deficient cells
Jennings, Lee D.,Kincaid, Scott L.,Wang, Yanong D.,Krishnamurthy, Girija,Beyer, Carl F.,McGinnis, John P.,Miranda, Miriam,Discafani, Carolyn M.,Rabindran, Sridhar K.
, p. 4731 - 4735 (2005)
A novel series of inhibitors of cancer cell proliferation, selective against p21 cell cycle checkpoint-disrupted cells vs. cells with intact p21 checkpoint, were identified by high-throughput screening. Optimization of both ends of the lead molecule to improve potency, using parallel synthesis and iterative design, is described. The 2-(1,4-dibenzodioxane)-substituted derivative 14 was identified as a highly selective and potent agent displaying an IC50 of 91 nM in the p21-deficient cell line.
Thiophene inhibitors of PDE4: Crystal structures show a second binding mode at the catalytic domain of PDE4D2
Nankervis, Jacob L.,Feil, Susanne C.,Hancock, Nancy C.,Zheng, Zhaohua,Ng, Hooi-Ling,Morton, Craig J.,Holien, Jessica K.,Ho, Patricia W.M.,Frazzetto, Mark M.,Jennings, Ian G.,Manallack, David T.,John Martin,Thompson, Philip E.,Parker, Michael W.
supporting information; experimental part, p. 7089 - 7093 (2012/01/06)
PDE4 inhibitors have been identified as therapeutic targets for a variety of conditions, particularly inflammatory diseases. We have serendipitously identified a novel class of phosphodiesterase 4 (PDE4) inhibitor during a study to discover antagonists of the parathyroid hormone receptor. X-ray crystallographic studies of PDE4D2 complexed to four potent inhibitors reveal the atomic details of how they inhibit the enzyme and a notable contrast to another recently reported thiophene-based inhibitor.
SYNTHESIS OF FULLY AROMATIC PYRIDOTHIENOPYRIMIDINE DERIVATIVES
Sauter, F.,Jordis, U.,Froehlich, J.,Gewald, K.,Grohmann, F.,Ahmed, E. K.
, p. 489 - 498 (2007/10/02)
Reaction of N-protected 4-piperidones with sulfur and cyanacetamide gave thienopyridine derivatives which were cyclized to tetrahydro-pyridothienopyrimidines.Subsequently the pyrido moiety of these products was aromatized.The prod
