Bioorganic & Medicinal Chemistry Letters 2009-08-15

Novel derivatives of ISO-1 as potent inhibitors of MIF biological function.

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

文献索引：Bioorg. Med. Chem. Lett. 19(16) , 4773-6, (2009)

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摘要

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.