Publication: Design, Synthesis, and Evaluation of Organic and Organometallic Pyrazoline Derivatives as Selective Dual COX-2/5-LOX Inhibitors and Potential Anticancer Agents
Design, Synthesis, and Evaluation of Organic and Organometallic Pyrazoline Derivatives as Selective Dual COX-2/5-LOX Inhibitors and Potential Anticancer Agents
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Navarrete, E., Cáceres M, T., Morales, P., Muñoz-Osses, M., Blacque, O., Mesdom, P., Cariou, K., Godoy, F., Gasser, G., Flores, E., & Mascayano, C. (2025). Design, Synthesis, and Evaluation of Organic and Organometallic Pyrazoline Derivatives as Selective Dual COX-2/5-LOX Inhibitors and Potential Anticancer Agents. Journal of Medicinal Chemistry, 69(2), 1387–1402. https://doi.org/10.1021/acs.jmedchem.5c02815
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Inspired by the structure of the anti-inflammatory drug Celecoxib, which is currently used in cancer prevention and treatment, we report the design, synthesis, and biological evaluation of organic and organometallic molecular hybrids based on pyrazolines (-). Structure-Activity Relationship (SAR) analyses showed that the combination of catechol-benzenesulfonamide in (organic) and (ferrocenyl) derivatives acts as potent and highly selective dual inhibitors (IC COX-2 = 4.58 and 2.88 μM; IC 5-LOX = 0.23 and 0.10 μM, respectively; evaluat
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Navarrete, E., Cáceres M, T., Morales, P., Muñoz-Osses, M., Blacque, O., Mesdom, P., Cariou, K., Godoy, F., Gasser, G., Flores, E., & Mascayano, C. (2025). Design, Synthesis, and Evaluation of Organic and Organometallic Pyrazoline Derivatives as Selective Dual COX-2/5-LOX Inhibitors and Potential Anticancer Agents. Journal of Medicinal Chemistry, 69(2), 1387–1402. https://doi.org/10.1021/acs.jmedchem.5c02815