- Identification and structure activity relationship of novel flavone derivatives that inhibit the production of nitric oxide and PGE2 in LPS-induced RAW 264.7 cells
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In an effort to identify novel anti-inflammatory compounds, a series of flavone derivatives were synthesized and biologically evaluated for their inhibitory effects on the production of nitric oxide (NO) and prostaglandin E2 (PGE2), representative pro-inflammatory mediators, in LPS-induced RAW 264.7 cells. Their structure-activity relationship was also investigated. In particular, we found that compound 3g displayed more potent inhibitory activities on PGE2 production, similar inhibitory activities on NO production and less weak cytotoxicity than luteolin, a natural flavone known as a potent anti-inflammatory agent.
- An, Ji-Young,Lee, Hwi-Ho,Shin, Ji-Sun,Yoo, Hyung-Seok,Park, Jong Seon,Son, Seung Hwan,Kim, Sang Won,Yu, Jihyun,Lee, Jun,Lee, Kyung-Tae,Kim, Nam-Jung
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- A versatile approach to flavones via a one-pot Pd(II)-catalyzed dehydrogenation/oxidative boron-Heck coupling sequence of chromanones
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A variety of flavones were expediently synthesized from readily accessible chromanones via a one-pot sequence involving Pd(ii)-catalyzed dehydrogenation and oxidative boron-Heck coupling with arylboronic acid pinacol esters. In particular, the use of arylboronic acid pinacol esters was found to significantly improve the yield of the reaction.
- Lee, Jun,Yu, Jihyun,Son, Seung Hwan,Heo, Jinyuk,Kim, Taelim,An, Ji-Young,Inn, Kyung-Soo,Kim, Nam-Jung
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p. 777 - 784
(2016/01/12)
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- Synthetic approach to flavanones and flavones via ligand-free palladium(ii)-catalyzed conjugate addition of arylboronic acids to chromones
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The remarkable catalytic effects of Fe(OTf)3 in the context of the Pd(ii)-catalyzed conjugate addition of arylboronic acids to chromones were observed to yield a variety of flavanones under mild conditions. The addition of catalytic amounts of DDQ and KNO2 to the reactions exclusively yielded flavone analogs. The reaction scope for the transformation was fairly broad, affording good yields of a wide range of flavanones and flavones, which are privileged structures in many biologically active compounds.
- Kim, Donghee,Ham, Kyungrok,Hong, Sungwoo
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experimental part
p. 7305 - 7312
(2012/09/22)
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