title: Synthesis and biological evaluation of novel thiazolidinedione analogues as 15-hydroxyprostaglandin dehydrogenase inhibitors.
abstract: Novel thiazolidinedione analogues as 15-hydroxyprostaglandin dehydrogenase (15-PGDH) inhibitors were synthesized. Compounds 2, 3, and 4 exhibited IC(50) of 25, 8, and 19 nM, respectively. They also significantly increased levels of PGE(2) in A549 cells. To assess the influence of 15-PGDH inhibitor on cochlear blood flow (CBF), 2 was applied intravenously to guinea pigs. It increased their CBFs. Scratch wounds were also analyzed in confluent monolayers of HaCaT cells. Cells exposed to 4 showed significantly improved wound healing with respect to a control.
authors.affiliation: Department of Polymer Science and Engineering, Chosun University, Gwangju 501-759, South Korea.
authors.forename: Ying
authors.initials: Y
authors.lastname: Wu
authors.forename: Sandeep
authors.initials: S
authors.lastname: Karna
authors.forename: Cheol Hee
authors.initials: CH
authors.lastname: Choi
authors.forename: Min
authors.initials: M
authors.lastname: Tong
authors.forename: Hsin-Hsiung
authors.initials: HH
authors.lastname: Tai
authors.forename: Dong Hee
authors.initials: DH
authors.lastname: Na
authors.forename: Chul Ho
authors.initials: CH
authors.lastname: Jang
authors.forename: Hoon
authors.initials: H
authors.lastname: Cho
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D003051:Cochlea / Q000098:blood supply / Q000187:drug effects; D051545:Cyclooxygenase 1 / Q000096:biosynthesis; D051546:Cyclooxygenase 2 / Q000096:biosynthesis; D015232:Dinoprostone / Q000096:biosynthesis; D006168:Guinea Pigs; D006801:Humans; D006911:Hydroxyprostaglandin Dehydrogenases / Q000037:antagonists & inhibitors*; D008297:Male; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000096:biosynthesis; D027361:Organic Anion Transporters / Q000096:biosynthesis; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014945:Wound Healing / Q000187:drug effects
chemical_list: D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D015232:Dinoprostone; D006911:Hydroxyprostaglandin Dehydrogenases; D027425:ATP-Binding Cassette, Sub-Family C Proteins; D027361:Organic Anion Transporters; D045162:Thiazolidinediones; C073492:ABCC4 protein, human; C503526:SLCO2A1 protein, human; C035859:15-hydroxyprostaglandin dehydrogenase