Dual cyclooxygenase-2 (COX-2)/5-lipoxygenase (5-LO) inhibitors are potential therapeutic agents for inflammatory diseases and for prostate cancer. CAY10416 is a dual COX-2/5-LO inhibitor with IC50 values of 50 and 3 nM, respectively.1 The selectivity of CAY10416 for COX is greater than 200-fold for COX-2 versus COX-1. COX-2/5-LO inhibitors such as CAY10416 are also apoptosis-inducing agents and are potentially useful in prostate cancer chemotherapy. In the PC3 human carcinoma cell line, CAY10416 exhibits a 45% inhibition of proliferation at 100 µM. In the LNCaP human carcinoma cell line, CAY10416 inhibits growth with an IC50 value of 83 µM.
1
Barbey, S., Goossens, L., Taverne, T., et al. Synthesis and activity of a new methoxytetrahydropyran derivative as dual cyclooxygenase-2/5-lipoxygenase inhibitor. Bioorg Med Chem Lett12779-782(2002).
Barbey, S., Goossens, L., Taverne, T., et al. Synthesis and activity of a new methoxytetrahydropyran derivative as dual cyclooxygenase-2/5-lipoxygenase inhibitor. Bioorg Med Chem Lett12779-782(2002).
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