3493-98-9Relevant academic research and scientific papers
A Scaffold-Hopping Strategy toward the Identification of Inhibitors of Cyclin G Associated Kinase
Wouters, Randy,Tian, Junjun,Herdewijn, Piet,De Jonghe, Steven
, p. 237 - 254 (2019/01/08)
We recently reported the discovery of isothiazolo[4,3-b]pyridine-based inhibitors of cyclin G associated kinase (GAK) displaying low nanomolar binding affinity for GAK and demonstrating broad-spectrum antiviral activity. To come up with novel core structures that act as GAK inhibitors, a scaffold-hopping approach was applied starting from two different isothiazolo[4,3-b]pyridines. In total, 13 novel 5,6- and 6,6-fused bicyclic heteroaromatic scaffolds were synthesized. Four of them displayed GAK affinity with Kd values in the low micromolar range that can serve as chemical starting points for the discovery of GAK inhibitors based on a different scaffold.
REACTIVITIES OF HETEROCYCLIC COMPOUNDS IN NITRATION. 5. KINETICS OF NITRATION OF 5-SUBSTITUTED 2-PICRYLAMINOPYRIDINES
Sharnin, G. P.,Falyakhov, I. F.,Khairutdinov, F. G.
, p. 1234 - 1238 (2007/10/02)
The kinetics of nitration of 5-bromo-, 5-chloro-, and 5-nitro-2-picrylaminopyridines in 80-96percent sulfuric acid were studied by a spectrophotometric method.The kinetic parameters of nitration were calculated.The UV spectra of the neutral and protonated forms in aqueous sulfuric acid solutions were identified.It was established that the indicated compounds are nitrated in the protonated form.The relative (as compared with benzene) rates of nitration were calculated.
