55115-79-2Relevant academic research and scientific papers
Synthesis and evaluation of pyrido-thieno-pyrimidines as potent and selective Cdc7 kinase inhibitors
Zhao, Chunlin,Tovar, Christian,Yin, Xuefeng,Xu, Qui,Todorov, Ivan T.,Vassilev, Lyubomir T.,Chen, Li
scheme or table, p. 319 - 323 (2011/02/26)
Cdc7 kinase plays a critical role in the regulation of DNA replication in eukaryotic cells and has been proposed as a target for cancer therapy. We have identified a class of Cdc7/Dbf4 inhibitors with a pyrido-thieno-pyrimidine core structure. Synthesis o
Tyrosine kinase inhibitors. 16. 6,5,6-Tricyclic benzothieno[3,2-d]pyrimidines and pyrimido[5,4-b]- and -[4,5- b]indoles as potent inhibitors of the epidermal growth factor receptor tyrosine kinase
Showalter, H. D. Hollis,Bridges, Alexander J.,Zhou, Hairong,Sercel, Anthony D.,McMichael, Amy,Fry, David W.
, p. 5464 - 5474 (2007/10/03)
Several elaborations of the fundamental anilinopyrimidine pharmacophore have been reported as potent and selective inhibitors of the epidermal growth factor receptor (EGFr) tyrosine kinase. This paper reports on a series of inhibitors whereby some 6,5-bicyclic heteroaromatic systems were fused through their C-2 and C-3 positions to this anilinopyrimidine pharmacophore. Although the resulting tricycles did not produce the enormous potency of some of the (5/6),6,6-bicyclic systems, the best of them had IC50s for the EGFr TK around 1 nM. Investigation of 4-position side chains in the indolopyrimidines confirmed that m-bromoaniline was an optimal substituent for potency. Investigation of substitution within the C-(benzo)ring of benzothienopyrimidines confirmed that introduction of an extra ring can change sharply the effects of substituents when compared to similar bicyclic nuclei, and only two substituents were found which even moderately enhanced inhibitory activity over the parent compound for this series.
Nucleophilic Displacements in Pyridine Rings
Dunn, A. D.,Norrie, R.
, p. 85 - 89 (2007/10/02)
The reactions of halopyridines containing an electron withdrawing group (-CN, -CO2R, -COMe, -NO2) with sulphur nucleophiles is reported.
