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Updated: Jun 21, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Novel derivatives of ISO-1 as potent inhibitors of MIF biological function
Sarala Balachandran1, Atish Rodge, Pradip K Gadekar
1Department of Medicinal Chemistry, Piramal Life Sciences, Off Western Express Highway, Goregaon (E), Mumbai 400 063, India. sarala.balachandran@piramal.com
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-1beta (IL-1beta) significantly better than ISO-1.
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