2. Academic Validation
  3. Novel derivatives of ISO-1 as potent inhibitors of MIF biological function

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

  • Bioorg Med Chem Lett. 2009 Aug 15;19(16):4773-6. doi: 10.1016/j.bmcl.2009.06.052.
Sarala Balachandran 1,  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
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Piramal Life Sciences, Off Western Express Highway, Goregaon (E), Mumbai 400 063, India. [email protected]
PMID: 19592246 DOI: 10.1016/j.bmcl.2009.06.052
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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