19228-91-2Relevant articles and documents
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.
N-Unsubstituted thienoisoindigos: preparation, molecular packing and ambipolar organic field-effect transistors
Yoo, Dongho,Hasegawa, Tsukasa,Ashizawa, Minoru,Kawamoto, Tadashi,Masunaga, Hiroyasu,Hikima, Takaaki,Matsumoto, Hidetoshi,Mori, Takehiko
supporting information, p. 2509 - 2512 (2017/03/17)
N-Unsubstituted thienoisoindigo (TIIG) and its diphenyl derivative (dph-TIIG) are synthesized by using a tert-butoxy carbonyl (t-Boc) group as a protecting group. TIIG has a stacking structure analogous to isoindigo, and dph-TIIG is a hybrid of brickwork
PYRROLOTRIAZINE INHIBITORS OF IRAK4 ACTIVITY
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Page/Page column 40, (2016/09/26)
The present invention relates to pyrrolotriazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
