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Literature DB >> 12036375

Structure-activity relationship studies of nordihydroguaiaretic acid inhibitors toward soybean, 12-human, and 15-human lipoxygenase.

Stephanie Whitman¹, Mikail Gezginci, Barbara N Timmermann, Theodore R Holman.

Abstract

Lipoxygenase (LO) is a biological target for many diseases such as asthma, atherosclerosis, and cancer. Our labs have synthesized and investigated nordihydroguaiaretic acid (NDGA) derivatives and have established that the reductive inhibition of soybean and 15-human LO can be affected by the strength of the electron-withdrawing substituents on the phenyl rings of NDGA. In addition, we have determined that hydrophobic NDGA derivatives activate 15-HLO, suggesting a hydrophobic allosteric site.

Entities: Chemical Disease Species

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Year: 2002 PMID： 12036375 DOI： 10.1021/jm0201262

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

31 in total

1. Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase.

Authors: Diane K Luci; J Brian Jameson; Adam Yasgar; Giovanni Diaz; Netra Joshi; Auric Kantz; Kate Markham; Steve Perry; Norine Kuhn; Jennifer Yeung; Edward H Kerns; Lena Schultz; Michael Holinstat; Jerry L Nadler; David A Taylor-Fishwick; Ajit Jadhav; Anton Simeonov; Theodore R Holman; David J Maloney
Journal: J Med Chem Date: 2014-01-06 Impact factor: 7.446

2. Discovery of potent and selective inhibitors of human platelet-type 12- lipoxygenase.

Authors: Victor Kenyon; Ganesha Rai; Ajit Jadhav; Lena Schultz; Michelle Armstrong; J Brian Jameson; Steven Perry; Netra Joshi; James M Bougie; William Leister; David A Taylor-Fishwick; Jerry L Nadler; Michael Holinstat; Anton Simeonov; David J Maloney; Theodore R Holman
Journal: J Med Chem Date: 2011-07-08 Impact factor: 7.446

3. Discovery of potent and selective inhibitors of human reticulocyte 15-lipoxygenase-1.

Authors: Ganesha Rai; Victor Kenyon; Ajit Jadhav; Lena Schultz; Michelle Armstrong; J Brian Jameson; Eric Hoobler; William Leister; Anton Simeonov; Theodore R Holman; David J Maloney
Journal: J Med Chem Date: 2010-10-28 Impact factor: 7.446

4. Pyridine and pyrimidine analogs of acetaminophen as inhibitors of lipid peroxidation and cyclooxygenase and lipoxygenase catalysis.

Authors: Tae-Gyu Nam; Susheel J Nara; Irène Zagol-Ikapitte; Thomas Cooper; Luca Valgimigli; John A Oates; Ned A Porter; Olivier Boutaud; Derek A Pratt
Journal: Org Biomol Chem Date: 2009-10-20 Impact factor: 3.876

Structure-activity relationship studies of nordihydroguaiaretic acid inhibitors toward soybean, 12-human, and 15-human lipoxygenase.

1. Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase.

2. Discovery of potent and selective inhibitors of human platelet-type 12- lipoxygenase.

3. Discovery of potent and selective inhibitors of human reticulocyte 15-lipoxygenase-1.

4. Pyridine and pyrimidine analogs of acetaminophen as inhibitors of lipid peroxidation and cyclooxygenase and lipoxygenase catalysis.

5. The potential of 12/15-lipoxygenase inhibitors in stroke therapy.

6. A novel inhibitor of 9-cis-epoxycarotenoid dioxygenase in abscisic acid biosynthesis in higher plants.

Review 7. Production of eicosanoids and other oxylipins by pathogenic eukaryotic microbes.

8. Synthesis, characterization, and anti-melanoma activity of tetra-O-substituted analogs of nordihydroguaiaretic acid.

9. Using enzyme assays to evaluate the structure and bioactivity of sponge-derived meroterpenes.

10. Novel lipoxygenase inhibitors as neuroprotective reagents.