Synthesis and biological evaluation of novel IM3829 (4-(2-cyclohexylethoxy)aniline) derivatives as potent radiosensitizers

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Abstract

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.

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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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