ISO-1的新型衍生物作为巨噬细胞迁移抑制因子（MIF）生物学功能的强效抑制剂
Novel derivatives of ISO-1 as potent inhibitors of MIF biological function.
作者信息
Balachandran Sarala, Rodge Atish, Gadekar Pradip K, Yadav Vitthal N, Kamath Divya, Chetrapal-Kunwar Anshu, Bhatt Pooja, Srinivasan Shaila, Sharma Somesh, Vishwakarma Ram A, Dagia Nilesh M
机构信息
Department of Medicinal Chemistry, Piramal Life Sciences, Off Western Express Highway, Goregaon (E), Mumbai 400 063, India.
出版信息
Bioorg Med Chem Lett. 2009 Aug 15;19(16):4773-6. doi: 10.1016/j.bmcl.2009.06.052. Epub 2009 Jun 17.
A series of novel 1,2,4-oxadiazole, phthalimide, amide and other derivatives of ISO-1 were synthesized and probed for inhibition of macrophage migration inhibitory factor (MIF) activity. Several compounds inhibited MIF enzymatic activity at levels better than ISO-1. Of note, compounds 7, 22, 23, 24, 25 and 27 inhibited the spontaneous secretion/release/recognition of MIF from freshly isolated human peripheral blood mononuclear cells and, more importantly, inhibited the MIF-induced production of interleukin-6 (IL-6) and/or interleukin-1beta (IL-1beta) significantly better than ISO-1.
合成了一系列新型的1,2,4-恶二唑、邻苯二甲酰亚胺、酰胺及其他ISO-1衍生物，并对其抑制巨噬细胞迁移抑制因子（MIF）活性进行了探究。几种化合物对MIF酶活性的抑制水平优于ISO-1。值得注意的是，化合物7、22、23、24、25和27抑制了新鲜分离的人外周血单核细胞中MIF的自发分泌/释放/识别，更重要的是，它们对MIF诱导的白细胞介素-6（IL-6）和/或白细胞介素-1β（IL-1β）产生的抑制作用明显优于ISO-1。
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