Derivatives of 1,2,4-Triazole Imines Acting as Dual iNOS and Tumor Cell Growth Inhibitors
Environmental Health Science
A set of 4-(R2-imino)-3-mercapto-5-(R1)-4H-1,2,4-triazoles derivatives were synthesized, characterized and evaluated for their ability to inhibit nitric oxide (NO) production in PAM212 mouse keratinocytes, which led to the discovery and the subsequent evaluation of their growth inhibitory cytotoxic potency toward that same mouse cell line together with a number of human cells lines (PC3, HT-29 and HeLa). Some limited SAR could be established for both NO production inhibition potency and growth inhibition cytotoxicity. Noticeably, the compounds designed to be nitrofurantoin mimics were the most potent anti-neoplastic agents.
Guillon, C., Vetrano, A. M., Saxena, J., Hunter, A., Verderone, G., Finetti, T. M., Wisnoski, J., DeMatteo, P. W., Rapp, R. D., Heindel, N. D., Joseph, L. B., Heck, D. E., & Laskin, J. D. (2020). Derivatives of 1,2,4-Triazole Imines Acting as Dual iNOS and Tumor Cell Growth Inhibitors. Bioorganic Chemistry, 103, 104128-104128. https://doi.org/10.1016/j.bioorg.2020.104128