A chrysin analog exhibited strong inhibitory activities against both PGE2 and NO production
A chrysin analog exhibited strong inhibitory activities against both PGE2 and NO production
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DOI：
10.1016/j.ejmech.2011.04.044
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发表时间：
2011-09-01
影响因子：
6.7
通讯作者：
Park, Haeil
中科院分区：
文献类型：
--
作者：
Che, Haiyan;Lim, Hyun;Park, Haeil
已经制备了许多8-取代的白杨素类似物，并评估了它们对环加氧酶2催化的前列腺素E-2和iNOS介导的NO产生的抑制活性。通过 8-碘-5,7-二甲氧基黄酮和烷基/芳烃硼酸的 Suzuki-Miyaura C-C 交叉偶联反应作为关键反应制备了类似物。在测试的类似物中，与白杨素相比，5,7-二羟基-8-(吡啶-4-基)黄酮 (3d) 对 COX-2 催化的 PGE(2) 和 iNOS 介导的 LPS 诱导的 RAW 264.7 细胞产生 NO 表现出强大的生物活性。 (C) 2011 Elsevier Masson SAS。版权所有。
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. (C) 2011 Elsevier Masson SAS. All rights reserved.