Literature DB >> 16682188

Critical modifications of the ISO-1 scaffold improve its potent inhibition of macrophage migration inhibitory factor (MIF) tautomerase activity.

Kai Fan Cheng1, Yousef Al-Abed.   

Abstract

Based on the scaffold of (S,R)-3-(4-hydroxyphenyl)-4,5-dihydro-5-isoxazole acetic acid methyl ester (ISO-1), an inhibitor of the proinflammatory cytokine MIF, two critical modifications and chiral resolution have significantly improved the potency of the inhibition. Compound (R)-17 is 20-fold more potent than ISO-1 and inhibits MIF tautomerase activity with an IC(50) of 550 nM.

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Year:  2006        PMID： 16682188     DOI： 10.1016/j.bmcl.2006.04.038

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


  13 in total

1.  Identification of Iguratimod as an Inhibitor of Macrophage Migration Inhibitory Factor (MIF) with Steroid-sparing Potential.

Authors:  Joshua Bloom; Christine Metz; Saisha Nalawade; Julian Casabar; Kai Fan Cheng; Mingzhu He; Barbara Sherry; Thomas Coleman; Thomas Forsthuber; Yousef Al-Abed
Journal:  J Biol Chem       Date:  2016-10-28       Impact factor: 5.157

2.  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

3.  Macrophage migration inhibitory factor mediates hypoxia-induced pulmonary hypertension.

Authors:  Yinzhong Zhang; Arunabh Talwar; Donna Tsang; Annette Bruchfeld; Ali Sadoughi; Maowen Hu; Kennedy Omonuwa; Kai Fan Cheng; Yousef Al-Abed; Edmund J Miller
Journal:  Mol Med       Date:  2012-03-27       Impact factor: 6.354

4.  Aza-derivatives of resveratrol are potent macrophage migration inhibitory factor inhibitors.

Authors:  Yoshihiko Fujita; Rafiqul Islam; Kazuko Sakai; Hiroyasu Kaneda; Kanae Kudo; Daisuke Tamura; Keiichi Aomatsu; Tomoyuki Nagai; Hidekazu Kimura; Kazuko Matsumoto; Marco A de Velasco; Tokuzo Arao; Tadashi Okawara; Kazuto Nishio
Journal:  Invest New Drugs       Date:  2011-09-13       Impact factor: 3.850

5.  A new therapeutic approach using a schizophyllan-based drug delivery system for inflammatory bowel disease.

Authors:  Hidetoshi Takedatsu; Keiichi Mitsuyama; Shinichi Mochizuki; Teppei Kobayashi; Kazuo Sakurai; Hiroshi Takeda; Yoshihide Fujiyama; Yoshikazu Koyama; Jun Nishihira; Michio Sata
Journal:  Mol Ther       Date:  2012-02-14       Impact factor: 11.454

6.  Phenolic hydrazones are potent inhibitors of macrophage migration inhibitory factor proinflammatory activity and survival improving agents in sepsis.

Authors:  Darrin R Dabideen; Kai Fan Cheng; Bayan Aljabari; Edmund J Miller; Valentin A Pavlov; Yousef Al-Abed
Journal:  J Med Chem       Date:  2007-03-27       Impact factor: 7.446

7.  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

8.  Macrophage Migration Inhibitory Factor (MIF) Makes Complex Contributions to Pain-Related Hyperactivity of Nociceptors after Spinal Cord Injury.

Authors:  Alexis G Bavencoffe; Emily A Spence; Michael Y Zhu; Anibal Garza-Carbajal; Kerry E Chu; Ona E Bloom; Carmen W Dessauer; Edgar T Walters
Journal:  J Neurosci       Date:  2022-05-23       Impact factor: 6.709

9.  Discovery of human macrophage migration inhibitory factor (MIF)-CD74 antagonists via virtual screening.

Authors:  Zoe Cournia; Lin Leng; Sunilkumar Gandavadi; Xin Du; Richard Bucala; William L Jorgensen
Journal:  J Med Chem       Date:  2009-01-22       Impact factor: 7.446

10.  Structural and functional characterization of a secreted hookworm Macrophage Migration Inhibitory Factor (MIF) that interacts with the human MIF receptor CD74.

Authors:  Yoonsang Cho; Brian F Jones; Jon J Vermeire; Lin Leng; Lisa DiFedele; Lisa M Harrison; Huabao Xiong; Yuen-Kwan Amy Kwong; Yibang Chen; Richard Bucala; Elias Lolis; Michael Cappello
Journal:  J Biol Chem       Date:  2007-06-13       Impact factor: 5.157
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