0000000001313682
AUTHOR
Francesco Ansideri
showing 4 related works from this author
Structural Optimization of a Pyridinylimidazole Scaffold: Shifting the Selectivity from p38α Mitogen-Activated Protein Kinase to c-Jun N-Terminal Kin…
2018
Starting from known p38α mitogen-activated protein kinase (MAPK) inhibitors, a series of inhibitors of the c-Jun N-terminal kinase (JNK) 3 was obtained. Altering the substitution pattern of the pyridinylimidazole scaffold proved to be effective in shifting the inhibitory activity from the original target p38α MAPK to the closely related JNK3. In particular, a significant improvement for JNK3 selectivity could be achieved by addressing the hydrophobic region I with a small methyl group. Furthermore, additional structural modifications permitted to explore structure–activity relationships. The most potent inhibitor 4-(4-methyl-2-(methylthio)-1H-imidazol-5-yl)-N-(4-morpholinophenyl)pyridin-2-a…
1-(3′,6′-Dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthen]-5-yl)-3-[4-({4-[1-(4-fluorophenyl)-1H-imidazol-5-yl]pyridin-2-yl}amino)phenyl]thiourea …
2016
The title compound, which crystallized as a methanol monosolvate, C41H27FN6O5S·CH3OH, was synthesized as a probe for a fluorescence polarization-based competition binding assay. The isobenzofuran fused-ring system is close to planar and orientated almost perpendicular to the central ring of the xanthene system. The dihedral angle between the benzene rings of the xanthene system is 10.0 (2)°, indicating a butterfly-like orientation. A short intramolecular C—F...π contact [F...π = 3.100 (4) Å and C—F...π = 139.9 (3)°] to the six-membered ring of the isobenzofuran system may influence the molecular conformation. The methanol solvent molecule is disordered over two orientations in a 0.6:0.4 rat…
CCDC 1824231: Experimental Crystal Structure Determination
2018
Related Article: Francesco Ansideri, Joana T. Macedo, Michael Eitel, Ahmed El-Gokha, Dhafer S. Zinad, Camilla Scarpellini, Mark Kudolo, Dieter Schollmeyer, Frank M. Boeckler, Bärbel S. Blaum, Stefan A. Laufer, and Pierre Koch|2018|ACS Omega|3|7809|doi:10.1021/acsomega.8b00668
CCDC 1917242: Experimental Crystal Structure Determination
2019
Related Article: Stanislav Andreev, Tatu Pantsar, Francesco Ansideri, Mark Kudolo, Michael Forster, Dieter Schollmeyer, Stefan A. Laufer, Pierre Koch|2019|Molecules|24|2331|doi:10.3390/molecules24122331