PMID- 24588120 OWN - NLM STAT- MEDLINE DCOM- 20150703 LR - 20191027 IS - 1875-6638 (Electronic) IS - 1573-4064 (Linking) VI - 10 IP - 7 DP - 2014 TI - Synthesis and biological evaluation of sulfonilamidothienopyrimidinone derivatives as novel anti-inflammatory agents. PG - 700-10 AB - Eight new sulfonilamidothienopyrimidinone derivatives (1-8) were synthesized and evaluated for their antiinflammatory activity on the human keratinocyte line NCTC 2544. The potential anti-inflammatory activity of the derivatives (1-8) was evaluated by determining, through Western blot, the expression of cyclooxygenase (COX)-2, inducible NO synthase (iNOS), intercellular adhesion molecule-1 (ICAM-1), and the release of prostaglandins (PG)E2 and interleukin- 8 (IL-8). Moreover, through ELISA assay, the release of monocyte chemoattractant protein-1 (MCP-1), and interleukin- 8 (IL-8) was analyzed. Our results demonstrated that the derivatives 3, 5, 6 and 8 act as excellent inhibitors of inflammatory markers: iNOS, COX-2, ICAM-1, MCP-1, and IL-8. These findings could be useful for the development of new drugs for the treatment of various inflammatory pathologies. FAU - Barone, Mariarita AU - Barone M FAU - Santagati, Andrea AU - Santagati A FAU - Graziano, Adriana C E AU - Graziano AC FAU - Fortuna, Cosimo G AU - Fortuna CG FAU - Ronsisvalle, Giuseppe AU - Ronsisvalle G FAU - Cardile, Venera AU - Cardile V AD - Department of Biomedical (Physiology), University of Catania, V.le A. Doria 6-95125 Catania, Italy. cardile@unict.it. LA - eng PT - Journal Article PL - Netherlands TA - Med Chem JT - Medicinal chemistry (Shariqah (United Arab Emirates)) JID - 101240303 RN - 0 (Anti-Inflammatory Agents, Non-Steroidal) RN - 0 (Bridged Bicyclo Compounds, Heterocyclic) RN - 0 (Sulfonamides) RN - 126547-89-5 (Intercellular Adhesion Molecule-1) RN - EC 1.14.13.39 (Nitric Oxide Synthase Type II) RN - EC 1.14.99.1 (Cyclooxygenase 2) SB - IM MH - Anti-Inflammatory Agents, Non-Steroidal/*chemical synthesis/chemistry/*pharmacology MH - Bridged Bicyclo Compounds, Heterocyclic/chemical synthesis/*chemistry/*pharmacology MH - Cell Proliferation/drug effects MH - Cell Survival/drug effects MH - Cells, Cultured MH - Cyclooxygenase 2/metabolism MH - Humans MH - Intercellular Adhesion Molecule-1/biosynthesis/metabolism MH - Molecular Structure MH - Nitric Oxide Synthase Type II/biosynthesis/metabolism MH - Sulfonamides/chemical synthesis/*chemistry/*pharmacology EDAT- 2014/03/05 06:00 MHDA- 2015/07/04 06:00 CRDT- 2014/03/05 06:00 PHST- 2013/07/17 00:00 [received] PHST- 2014/02/11 00:00 [revised] PHST- 2014/02/11 00:00 [accepted] PHST- 2014/03/05 06:00 [entrez] PHST- 2014/03/05 06:00 [pubmed] PHST- 2015/07/04 06:00 [medline] AID - MC-EPUB-59399 [pii] AID - 10.2174/1573406410666140228152807 [doi] PST - ppublish SO - Med Chem. 2014;10(7):700-10. doi: 10.2174/1573406410666140228152807.