6-Aryl-pyrazolo[3,4-b]pyridines: Potent inhibitors of glycogen synthase kinase-3 (GSK-3)

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 18, 2003, Pages 3055-3057

  Witherington, Jason ^a   Bordas, Vincent ^a   Gaiba, Alessandra ^a   Garton, Neil S ^a   Naylor, Antoinette ^a   Rawlings, Anthony D ^a   Slingsby, Brian P ^a   Smith, David G ^a   Takle, Andrew K ^a   Ward, Robert W ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

GLYCOGEN SYNTHASE KINASE 3; PHOSPHOTRANSFERASE INHIBITOR; PYRIDINE DERIVATIVE;

ARTICLE; DRUG IDENTIFICATION; DRUG POTENTIATION; X RAY CRYSTALLOGRAPHY;

EID: 12444280004     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00645-0     Document Type: Article

References (18)

1. (a) Leloir L.F., Olavaria S.H., Goldenberg S.H., Carminatti H. Arch. Biochem. Biophys. 81:1959;508.
2. (b) Mandarino L., Wright K., Verity L., Nichols J., Bell J., Kolterman O., Beck-Nielsen H. J. Clin. Invest. 80:1987;655.
3. (c) Roach P. FASEB J. 4:1990;2961.
4. (d) Skurat A.V., Roach P.J. Biochem. J. 313:1996;45
5. (e) Zhang W., DePaoli-Roach A.A., Roach P.J. Arch. Biochem. Biophys. 304:1993;219.
6. (f) Eldar-Finkelmann H., Argast G.M., Foord O., Fischer E.H., Krebs E.G. Proc. Natl. Acad. Sci. U.S.A. 93:1996;10228.
7. (g) DeFronzo R.A., Bonadonna R.C., Ferrannini E. Diabetes Care. 15:1992;318.
8. (h) Thorburn A.W., Gumbiner B., Bulacan F., Wallace P., Henry R.R. J. Clin. Invest. 85:1990;522.
9. (j) Beck-Nielsen H., Vaag A., Damsbo P., Handberg A., Neilsen O.H., Henriksen J.E., Thye-Ronn P. Diabetes Care. 15:1992;418.
10. (k) Bogardus C., Lillioja S., Stone K., Mott D. J. Clin. Invest. 73:1984;1185.
11. (l) Lovestone S., Reynolds C.H., Latimer D., Davis D.R., Anderton B.H., Gallo J.-M., Hanger D., Mulot S., Marquardt B. Curr. Biol. 4:1994;1077.
12. (m) Pap M., Cooper G.M. J. Biol. Chem. 273:1998;19929.
13. Klein P.S., Melton D.A. Proc. Natl. Acad. Sci. U.S.A. 93:1996;8455.
14. (a) Witherington, J.; Bordas, V.; Garland, S. L.; Hickey, D. M.; Ife, R. J.; Liddle, J.; Saunders, M.; Smith, D. G. Bioorg. Med. Chem. Lett. In press.
15. (b) Witherington, J.; Bordas, V.; Haigh D.; Hickey, D. M.; Ife, R. J.; Rawlings, A. R.; Slingsby, B.; Smith, D. G.; Ward, R. Bioorg. Med. Chem. Lett. In press.
16. Results are a mean of at least two determinations run in duplicate (n=4) and are given as mean. Mean±SEM are also quoted for compounds of specific interest.
17. Assay conditions described in ref 2a.
18. All novel compounds gave satisfactory analytical data in full agreement with their proposed structures.