Literature DB >> 19592246

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

Sarala Balachandran1, 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.   

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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Year:  2009        PMID: 19592246     DOI: 10.1016/j.bmcl.2009.06.052

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

1.  Advances and Insights for Small Molecule Inhibition of Macrophage Migration Inhibitory Factor.

Authors:  Vinay Trivedi-Parmar; William L Jorgensen
Journal:  J Med Chem       Date:  2018-06-04       Impact factor: 7.446

2.  Design, synthesis, and protein crystallography of biaryltriazoles as potent tautomerase inhibitors of macrophage migration inhibitory factor.

Authors:  Pawel Dziedzic; José A Cisneros; Michael J Robertson; Alissa A Hare; Nadia E Danford; Richard H G Baxter; William L Jorgensen
Journal:  J Am Chem Soc       Date:  2015-02-20       Impact factor: 15.419

3.  Identification and characterization of novel classes of macrophage migration inhibitory factor (MIF) inhibitors with distinct mechanisms of action.

Authors:  Hajer Ouertatani-Sakouhi; Farah El-Turk; Bruno Fauvet; Min-Kyu Cho; Damla Pinar Karpinar; Didier Le Roy; Manfred Dewor; Thierry Roger; Jürgen Bernhagen; Thierry Calandra; Markus Zweckstetter; Hilal A Lashuel
Journal:  J Biol Chem       Date:  2010-06-01       Impact factor: 5.157

4.  Overexpression of macrophage migration inhibitory factor in adenoid cystic carcinoma: correlation with enhanced metastatic potential.

Authors:  Hui Liu; Gang Chen; Wei Zhang; Jun-Yi Zhu; Zhao-Quan Lin; Zhong-Cheng Gong; Feng-Qin Wang; Jun Jia; Zhi-Jun Sun; Yi-Fang Zhao
Journal:  J Cancer Res Clin Oncol       Date:  2012-10-12       Impact factor: 4.553

5.  Brain miffed by macrophage migration inhibitory factor.

Authors:  Nic E Savaskan; Günter Fingerle-Rowson; Michael Buchfelder; Ilker Y Eyüpoglu
Journal:  Int J Cell Biol       Date:  2012-09-03

6.  Macrophage migration inhibitory factor mediates peripheral nerve injury-induced hypersensitivity by curbing dopaminergic descending inhibition.

Authors:  Xian Wang; Shaolei Ma; Haibo Wu; Xiaofeng Shen; Shiqin Xu; Xirong Guo; Maria L Bolick; Shizheng Wu; Fuzhou Wang
Journal:  Exp Mol Med       Date:  2018-02-16       Impact factor: 8.718

7.  A Fluorescence Polarization Assay for Binding to Macrophage Migration Inhibitory Factor and Crystal Structures for Complexes of Two Potent Inhibitors.

Authors:  José A Cisneros; Michael J Robertson; Margarita Valhondo; William L Jorgensen
Journal:  J Am Chem Soc       Date:  2016-06-28       Impact factor: 15.419

  7 in total

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