Novel derivatives of ISO-1 as potent inhibitors of MIF biological function |
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| Authors: | Sarala Balachandran Atish Rodge Pradip K Gadekar Vitthal N Yadav Divya Kamath Anshu Chetrapal-Kunwar Pooja Bhatt Shaila Srinivasan Somesh Sharma Ram A Vishwakarma Nilesh M Dagia |
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| Institution: | 1. Department of Medicinal Chemistry, Piramal Life Sciences, 1 Nirlon Complex, Off Western Express Highway, Goregaon (E), Mumbai 400 063, India;2. Department of Pharmacology, Piramal Life Sciences, 1 Nirlon Complex, Off Western Express Highway, Goregaon (E), Mumbai 400 063, India |
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| Abstract: | 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-1β (IL-1β) significantly better than ISO-1. |
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