A substituted quinoline with diverse biological activities
CMS121 is a substituted quinoline that has neuroprotective, anti-inflammatory, antioxidative, and renoprotective activities.[1][2][3] It maintains glutathione (GSH) levels in HT22 mouse hippocampal cells in vitro in the presence of glutamate, induces differentiation of PC12 cells, prevents LPS-induced N9 microglial activation by 82% in N9 microglia, and scavenges free radicals in a Trolox equivalent activity concentration (TEAC) assay.[1] CMS121 protects against ischemia and oxytosis in phenotypic screens in HT22 cells in vitro with EC50 values of 7 and 200 nM for preventing iodoacetic acid- or glutamate-induced cell death, respectively.[2]? It is also renoprotective, decreasing kidney weight loss and decreasing the expression of TNF-α, caspase-1, and inducible nitric oxide synthase (iNOS) in a SAMP8 mouse model of chronic kidney disease associated with rapid aging when administered at a dose of 10 mg/kg per day starting at nine months of age.[3]
Reference:
[1]. Chiruta, C., Schubert, D., Dargusch, R., et al. Chemical modification of the multi-target neuroprotective compound fisetin. J. Med. Chem. 55(1), 378-389 (2012).
[2]. Prior, M., Chiruta, C., Currais, A., et al. Back to the future with phenotypic screening. ACS Chem Neurosci. 5(7), 503-513 (2014).
[3]. Currais, A., Maher, P., Schubert, D., et al. Prevention and treatment of aging and neurodegenerative diseases. (2017).
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