Download MendeleyThe development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production.
Sabat, M., Vanrens, J.C., Clark, M.P., Brugel, T.A., Maier, J., Bookland, R.G., Laufersweiler, M.J., Laughlin, S.K., Golebiowski, A., De, B., Hsieh, L.C., Walter, R.L., Mekel, M.J., Janusz, M.J.(2006) Bioorg Med Chem Lett 16: 4360-4365
- PubMed: 16750367
- DOI: https://doi.org/10.1016/j.bmcl.2006.05.050
- Primary Citation of Related Structures:
2GTM, 2GTN - PubMed Abstract:
A series of C-2, C-8, and N-9 trisubstituted purine based inhibitors of TNF-alpha production are described. The most potent analogs showed low nanomolar activity against LPS-induced TNF-alpha production in a THP-1 cell based assay. The SAR of the series was optimized with the aid of X-ray co-crystal structures of these inhibitors bound with mutated p38 (mp38).
Organizational Affiliation:
Procter and Gamble Pharmaceuticals, Health Care Research Center, Mason, OH 45040, USA. [email protected]
