Nuclear factor-erythroid 2-related factor 2 (Nrf2) regulates the expression of over 200 genes of antioxidant and phase II drug-metabolizing enzymes, and is highly expressed in non-small cell lung cancer (NSCLC). Nine derivatives of 4-(2-cyclohexylethoxy)aniline were designed. Our previous study demonstrated that IM3829 increases radiosensitivity of several lung cancer cells in vitro and in vivo. Here, biological effects of IM3829 derivatives (2a-2i) were evaluated. Compound 2g derivative effectively inhibits mRNA and protein expression of Nrf2 and HO-1. In addition, we observed over two fold enhancement in IR-induced cell death, from 2.90 ± 0.22 to 6.02 ± 0.87, in H1299 cancer cell-line. Among the nine derivatives, compound 2g derivative exhibited the highest enhancement of radiosensitizing effect via inhibition of Nrf2 activity.
CITATION STYLE
Ahn, J., Nam, K. Y., Lee, S. L. O., Ryu, H., Choi, H. K., Jie, J., & Song. (2014). Synthesis and biological evaluation of novel IM3829 (4-(2-cyclohexylethoxy)aniline) derivatives as potent radiosensitizers. Bulletin of the Korean Chemical Society, 35(12), 3623–3626. https://doi.org/10.5012/bkcs.2014.35.12.3623
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