合成和评价新型色酮类似物对白细胞介素-5 的抑制活性。
Synthesis and evaluation of novel chromone analogs for their inhibitory activity against interleukin-5.
机构信息
College of Pharmacy and Institute of Drug Research and Development, Chungnam, National University, Daejeon 305-764, Republic of Korea.
出版信息
Eur J Med Chem. 2010 Jun;45(6):2531-6. doi: 10.1016/j.ejmech.2010.02.041. Epub 2010 Feb 20.
A novel series of chromone analogs were synthesized and evaluated for their inhibitory activity against interleukin-5. Among them compounds 5-Cyclohexylmethoxy-3-(4-hydroxybenzyl)-4H-chromen-4-one (6a, 98% inhibition at 30 microM, IC50<3.0 microM) and 5-Cyclohyxylmethoxy-3-(hydroxymethyl)-4H-chromen-4-one (8a, 84% inhibition at 30 microM, IC50=7.6 microM) showed most potent activity. The structural requirement of chromone analogs possessing the inhibitory activity against IL-5 could be summarized as: (i) importance of hydrophobic group such as cyclohexylmethoxy at 5th position of ring A, (ii) requirement of ring B with small size of hydrogen bonding group with electron donating property such as phenolic hydroxyl group at 4th position and (iii) planarity of the chromen-4-one ring.
新型色酮类似物被合成并评估了它们对白细胞介素-5 的抑制活性。其中，化合物 5-环己基甲氧基-3-(4-羟基苄基)-4H-色烯-4-酮（6a，在 30μM 时抑制率为 98%，IC50<3.0μM）和 5-环己基甲氧基-3-(羟甲基)-4H-色烯-4-酮（8a，在 30μM 时抑制率为 84%，IC50=7.6μM）表现出最强的活性。具有抑制白细胞介素-5 活性的色酮类似物的结构要求可以概括为：（i）A 环 5 位上的环己基甲氧基等疏水性基团的重要性，（ii）B 环上具有小的氢键供电子基团如 4 位上的酚羟基的要求，和（iii）色烯-4-酮环的平面性。
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