title: Discovery of 2-phenyl-3-sulfonylphenyl-indole derivatives as a new class of selective COX-2 inhibitors.
abstract: 2-Sulfonylphenyl-3-phenyl-indole derivatives have been reported to be highly potent and selective COX-2 inhibitors previously. In this paper, the regio-isomeric analogues-2-phenyl-3-sulfonylphenyl-indoles were identified as potent and selective COX-2 inhibitors. This work led to the discovery of compounds 4a and 8a possessing higher activity than Celecoxib on cellular assay.
authors.affiliation: Department of Synthetic Medicinal Chemistry, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, PR China.
authors.forename: Wenhui
authors.initials: W
authors.lastname: Hu
authors.forename: Zongru
authors.initials: Z
authors.lastname: Guo
authors.forename: Xiang
authors.initials: X
authors.lastname: Yi
authors.forename: Changbin
authors.initials: C
authors.lastname: Guo
authors.forename: Fengming
authors.initials: F
authors.lastname: Chu
authors.forename: Guifang
authors.initials: G
authors.lastname: Cheng
mesh_terms: D000818:Animals; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000145:classification / Q000494:pharmacology*; D007211:Indoles / Q000138:chemical synthesis* / Q000145:classification / Q000494:pharmacology*; D007527:Isoenzymes / Q000037:antagonists & inhibitors*; D017737:Macrophages, Peritoneal / Q000201:enzymology; D008297:Male; D008565:Membrane Proteins; D051379:Mice; D008810:Mice, Inbred C57BL; D015394:Molecular Structure; D011451:Prostaglandin-Endoperoxide Synthases
chemical_list: C488638:2-phenyl-3-sulfonylphenyl-indole; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007211:Indoles; D007527:Isoenzymes; D008565:Membrane Proteins; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D011451:Prostaglandin-Endoperoxide Synthases; C496512:Ptgs1 protein, mouse