title: 2,3-Diarylbenzopyran derivatives as a novel class of selective cyclooxygenase-2 inhibitors.
abstract: A new series of cyclooxygenase-2(COX-2) inhibitors with naturally occurring flavone as the main skeleton has been synthesized and their biological activities were evaluated for cyclooxygenase inhibitory activity. Rational structural modifications were applied to potent COX-2 inhibitors to obtain the desired pharmacokinetic profiles for improved oral anti-inflammatory activity.
authors.affiliation: Drug Discovery, AmorePacific Corporation R&D Center, 314-1 Bora-ri, Kiheung-eup, Yongin-si, Kyounggi-do 449-729, South Korea. yhjoo@pacific.co.kr
authors.forename: Yung Hyup
authors.initials: YH
authors.lastname: Hyup
authors.forename: Jin Kwan
authors.initials: JK
authors.lastname: Kwan
authors.forename: Seon-Hwa
authors.initials: SH
authors.lastname: Kang
authors.forename: Min-Soo
authors.initials: MS
authors.lastname: Noh
authors.forename: Jun-Yong
authors.initials: JY
authors.lastname: Ha
authors.forename: Jin Kyu
authors.initials: JK
authors.lastname: Kyu
authors.forename: Kyung Min
authors.initials: KM
authors.lastname: Min
authors.forename: Chang Hoon
authors.initials: CH
authors.lastname: Hoon
authors.forename: Shin
authors.initials: S
authors.lastname: Chung
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D001578:Benzopyrans / Q000138:chemical synthesis* / Q000494:pharmacology*; D002351:Carrageenan; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D007202:Indicators and Reagents; D007527:Isoenzymes / Q000378:metabolism*; D008297:Male; D008565:Membrane Proteins; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D001578:Benzopyrans; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007202:Indicators and Reagents; D007527:Isoenzymes; D008565:Membrane Proteins; D002351:Carrageenan; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D011451:Prostaglandin-Endoperoxide Synthases; C496513:Ptgs1 protein, rat