Department of Chemistry, Lehigh University, Bethlehem, PA 18015, USA.
Department of Environmental & Occupational Health, Environmental and Occupational Health Sciences Institute, Rutgers University School of Public Health, Piscataway, NJ 08854, USA.
Bioorg Chem. 2020 Oct;103:104128. doi: 10.1016/j.bioorg.2020.104128. Epub 2020 Jul 22.
A set of 4-(R-imino)-3-mercapto-5-(R)-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.
一组 4-(R-亚氨基)-3-巯基-5-(R)-4H-1,2,4-三唑衍生物被合成、表征，并评估其抑制 PAM212 小鼠角质细胞中一氧化氮（NO）产生的能力，这导致了对同一小鼠细胞系以及一些人类细胞系（PC3、HT-29 和 HeLa）的生长抑制细胞毒性潜力的发现和随后的评估。可以为 NO 产生抑制效力和生长抑制细胞毒性建立一些有限的 SAR。值得注意的是，设计为呋喃妥因类似物的化合物是最有效的抗肿瘤药物。
