- A Scaffold-Hopping Strategy toward the Identification of Inhibitors of Cyclin G Associated Kinase
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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.
- Wouters, Randy,Tian, Junjun,Herdewijn, Piet,De Jonghe, Steven
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p. 237 - 254
(2019/01/08)
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- 2-ALKENYL-3-AMINOTHIOPHENE DERIVATIVE AND METHOD FOR PRODUCING THE SAME
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Disclosed is a method for commercially producing 2-alkenyl-3-aminothiophene derivatives, which are useful as intermediates for agricultural chemicals, at low cost. Specifically disclosed is a method for introducing alkenyl groups into the 2-position of 3-aminothiophene derivatives by reacting 3-aminothiophene derivatives represented by the general formula (2) below or salts thereof with a ketone represented by the general formula (1) below without using a protecting group. Also specifically disclosed are 2-alkenyl-3-aminothiophene derivatives (3a) to (3d) which are useful as intermediates for agricultural chemicals,
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Page/Page column 12
(2009/01/24)
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- SUBSTITUTED THIENOPYRIDONE COMPOUNDS WITH ANTIBACTERIAL ACTIVITY
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Novel bicyclic heteroaromatic compounds are provided that are inhibitors of bacterial methionyl tRNA synthetase (MetRS). Compounds of the invention generally have a left hand side chroman group or left hand side tetrahydroquinoline group and a right hand
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Page/Page column 18
(2008/06/13)
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- Nouvelle synthese et etude de la stabilite de l'amino-3 thiophene
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A new synthesis of 3-aminothiophene is proposed starting from 3-thenoic acid via isopropyl 3-thienylcarbamate as intermediate.Thermal decomposition of this latter in alkaline medium gives 3-aminothiophene.NMR and mass spectral studies revealed that the instability of the amine is due to its polymerisation via thwe formation of the dimer di-3-thienylamine and the trimer tri-3-thienylamine.
- Rault, S.,Cugnon de Sevricourt, M.,Robba, M.
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p. 205 - 208
(2007/10/02)
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