A chrysin analog exhibited strong inhibitory activities against both PGE(2) and NO production

作者：Che Haiyan; Lim Hyun; Kim Hyun Pyo; Park Haeil^*

来源：European Journal of Medicinal Chemistry, 2011, 46(9): 4657-4660.

DOI：10.1016/j.ejmech.2011.04.044

• 8-Substituted chrysin analogs
• Wogonin
• Inflammation
• PGE(2)
• NO
• Suzuki-Miyaura reaction

A number of 8-substituted chrysin analogs have been prepared and evaluated for their inhibitory activities of cyclooxygenase-2 catalyzed prostaglandin E-2 and iNOS-mediated NO production. Analogs were prepared via Suzuki-Miyaura C-C cross coupling reaction of 8-iodo-5,7-dimethoxyflavone and alkyl/areneboronic acids as a key reaction. Among the analogs tested, 5,7-dihydroxy-8-(pyridine-4-yl) flavone (3d) showed strong biological activities against COX-2 catalyzed PGE(2) and iNOS-mediated NO production from LPS-induced RAW 264.7 cells compared to those of chrysin.

• 出版日期2011-9