ISO-1支架的关键修饰提高了其对巨噬细胞迁移抑制因子（MIF）互变异构酶活性的有效抑制作用。
Critical modifications of the ISO-1 scaffold improve its potent inhibition of macrophage migration inhibitory factor (MIF) tautomerase activity.
作者信息
Cheng Kai Fan, Al-Abed Yousef
机构信息
Department of Medicinal Chemistry, The Feinstein Institute for Medical Research, North Shore-LIJ Health System, 350 Community Drive, Manhasset, NY 11030, USA.
出版信息
Bioorg Med Chem Lett. 2006 Jul 1;16(13):3376-9. doi: 10.1016/j.bmcl.2006.04.038. Epub 2006 May 6.
Based on the scaffold of (S,R)-3-(4-hydroxyphenyl)-4,5-dihydro-5-isoxazole acetic acid methyl ester (ISO-1), an inhibitor of the proinflammatory cytokine MIF, two critical modifications and chiral resolution have significantly improved the potency of the inhibition. Compound (R)-17 is 20-fold more potent than ISO-1 and inhibits MIF tautomerase activity with an IC(50) of 550 nM.
基于促炎细胞因子MIF的抑制剂（S，R）-3-（4-羟基苯基）-4，5-二氢-5-异恶唑乙酸甲酯（ISO-1）的支架结构，两项关键修饰和手性拆分显著提高了抑制效力。化合物（R）-17的效力比ISO-1高20倍，以550 nM的IC（50）抑制MIF互变异构酶活性。
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