In Vitro Cytostatic Effect on Tumor Cells by Carborane‐Based Dual Cyclooxygenase‐2 and 5‐Lipoxygenase Inhibitors
نویسندگان
چکیده
Abstract The selective inhibition of enzymes that catalyze the conversion arachidonic acid to inflammatory eicosanoids represents a promising approach for cancer therapy. This study, therefore, focuses on incorporation metabolically stable, sterically demanding, and hydrophobic carboranes into existing dual cycloxygenase‐2 (COX‐2)/5‐lipoxygenase (5‐LO) inhibitors are key in biosynthesis eicosanoids. Here, first carborane‐containing COX‐2/5‐LO derived from RWJ‐63556 presented. replacement fluorophenyl moiety by meta ‐ or para ‐carborane resulted five derivatives 3 , 6 9 13 17 show high inhibitory activities toward COX‐2 5‐LO vitro. Cell viability studies A375 melanoma cell line revealed derivative shows higher anticancer activity compared based accumulation lipid droplets cells due blockage pathways, indicating design potent inhibitors.
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ژورنال
عنوان ژورنال: Advanced therapeutics
سال: 2023
ISSN: ['2366-3987']
DOI: https://doi.org/10.1002/adtp.202200252