Results 221 to 230 of about 43,549 (263)

Novel bishydroxamic acids as 5-lipoxygenase inhibitors

Bioorganic & Medicinal Chemistry, 1994
Two series of novel bishydroxamic acids 2 and 3 (types A and B) were synthesized and tested for inhibition of 5-lipoxygenase from rat basophile leukemia (RBL) cells. Both series were potent inhibitors of the isolated enzyme but only the type B reverse hydroxamic acids possessed significant oral activity. The most potent compound, orally, was 3a, [IC50 =
K A, Ohemeng, V N, Nguyen, C F, Schwender, M, Singer, M, Steber, J, Ansell, W, Hageman   +6 more
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Arachidonate 5-lipoxygenase and its new inhibitors

Journal of Allergy and Clinical Immunology, 1984
The 5-lipoxygenases of guinea pig peritoneal polymorphonuclear leukocytes and of rat basophilic leukemia cells have been solubilized, purified partially by affinity chromatography, and shown to convert arachidonic acid principally to 5-hydroperoxy-6,8,11,14- eicosatetraenoic acid.
S, Yamamoto, T, Yoshimoto, M, Furukawa, T, Horie, S, Watanabe-Kohno   +4 more
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Inhibitors of platelet lipoxygenase from Ponkan fruit

Phytochemistry, 2001
An activity-guided separation for inhibitors of rat platelet 12-lipoxygenase led to the isolation of two compounds, 4-O-feruloyl-5-O-caffeoylquinic acid (IC50; 5.5 microM) and methyl 4-O-feruloyl-5-O-caffeoylquinate (IC50; 1.9 microM) from the peel of Ponkan fruit (Citrus reticulata).
Y, Nogata, K, Sekiya, H, Ohta, K, Kusumoto, T, Ishizu   +4 more
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Lipoxygenase inhibitors prevent urological cancer cell growth

International Journal of Molecular Medicine, 2004
Recent studies have demonstrated that lipoxygenase (LOX) inhibitor induces growth arrest of cancer cells through apoptosis. In this study, we examined the effects of LOX inhibitors on cell proliferation in renal cell carcinoma (RCC), bladder tumor (BT), and prostate cancer (PC) cell lines. We investigated the inhibitory effect of LOX inhibitors, 5-, 12-
Masahide, Matsuyama, Rikio, Yoshimura, Kenji, Tsuchida, Yoshiaki, Takemoto, Yoshihiro, Segawa, Toshiaki, Shinnka, Yutaka, Kawahito, Hajime, Sano, Tatsuya, Nakatani   +8 more
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Flavonoids: Potent inhibitors of arachidonate 5-lipoxygenase

Biochemical and Biophysical Research Communications, 1983
Various flavonoids were found to be relatively selective inhibitors of arachidonate 5-lipoxygenase which initiates the biosynthesis of leukotrienes with the activity of slow reacting substance of anaphylaxis. Cirsiliol (3',4',5-trihydroxy-6,7-dimethoxyflavone) was most potent, and the enzyme partially purified from rat basophilic leukemia cells was ...
T, Yoshimoto, M, Furukawa, S, Yamamoto, T, Horie, S, Watanabe-Kohno   +4 more
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Comparative Biochemistry of Lipoxygenase Inhibitors

1985
This chapter describes some studies on the mechanism of 5-lipoxygenase regulation and inhibition and then presents an overview of lipoxygenase inhibitors that are active against intact-cell, broken-cell, and purifed enzymes from a variety of sources.
Robert W. Egan, Paul H. Gale
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Synthesis of new sulfonamides as lipoxygenase inhibitors

Bioorganic & Medicinal Chemistry, 2012
The present study describes a convenient method for the synthesis of new lipoxygenase inhibitors, 4-(toluene-4-sulfonylamino)-benzoic acids from p-amino benzoic acid. Reaction of p-amino benzoic acid with p-toluenesulfonyl chloride provided thirteen N- and O-alkylation products 4a-4m in moderate to good yields.
Ghulam, Mustafa, Islam Ullah, Khan, Muhammad, Ashraf, Iftikhar, Afzal, Sohail Anjum, Shahzad, Muhammad, Shafiq   +5 more
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Substituted coumarins as potent 5-lipoxygenase inhibitors

Bioorganic & Medicinal Chemistry Letters, 2006
Leukotriene biosynthesis inhibitors have potential as therapeutic agents for asthma and inflammatory diseases. A novel series of substituted coumarin derivatives has been synthesized and the structure-activity relationship was evaluated with respect to their ability to inhibit the formation of leukotrienes via the human 5-lipoxygenase enzyme.
Erich L, Grimm, Christine, Brideau, Nathalie, Chauret, Chi-Chung, Chan, Daniel, Delorme, Yves, Ducharme, Diane, Ethier, Jean-Pierre, Falgueyret, Richard W, Friesen, Jocelyne, Guay, Pierre, Hamel, Denis, Riendeau, Chantal, Soucy-Breau, Philip, Tagari, Yves, Girard   +14 more
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Catechol based inhibitors of 15-lipoxygenase

Bioorganic & Medicinal Chemistry Letters, 1996
Abstract A potent 15-lipoxygenase (15-LO) inhibitor, compound 6 , was identified by mass screening the Parke-Davis compound portfolio. The active moiety of compound 6 was determined to be the catechol functionality. Additional analogs were prepared and analyzed for inhibitory activity against 5-, 12-, and 15- lipoxygenase.
Bradley D. Tait, Richard D. Dyer, Bruce J. Auerbach, Dirk Bornemeier, Linda Guilds-Zamarka, Maritza Oxender, Bruce D. Roth, Bharat K. Trivedi, Joseph A. Cornicelli   +8 more
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Vinylogous hydroxamic acids: 5-lipoxygenase inhibitors

Bioorganic & Medicinal Chemistry Letters, 1992
Abstract Vinylogous hydroxamic acids were prepared as inhibitors of 5-lipoxygenase. The synthesis and preliminary SAR of these relatively unexplored compounds are described. These compounds are potent 5-lipoxygenase inhibitors which do not inhibit other enzymes of the arachidonic acid cascade.
Stephen W. Wright, Donald J. Pinto, Susan R. Sherk, Alicia M. Green, Ronald L. Magolda   +4 more
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