Program of Biotechnology, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand.
Bioorg Med Chem Lett. 2013 Nov 15;23(22):6156-60. doi: 10.1016/j.bmcl.2013.09.004. Epub 2013 Sep 8.
Overcoming drug resistance with remarkable cytotoxic activity by anthracene-9,10-dione derivatives would offer a potential therapeutic strategy. In this study, we report the synthesis and the cytotoxicity of a novel set of anthraquninones. (4-(4-Aminobenzylamino)-9,10-dioxo-9,10-dihydroanthracen-1-yl-4-methylbenzenesulfonate) (3) has excellent in vitro cytotoxicity against doxorubicin-resistant cancer cell line (IC50=0.8 μM), 20-fold higher than doxorubicin. The cytotoxic effect via G2/M arrest does not appear to be ROS.
通过蒽醌-9,10-二酮衍生物克服耐药性具有显著的细胞毒性活性，将提供一种潜在的治疗策略。在本研究中，我们报告了一组新型蒽醌酮的合成和细胞毒性。（4-（4-氨基苄基氨基）-9,10-二氧代-9,10-二氢蒽-1-基-4-甲基苯磺酸盐）（3）对阿霉素耐药癌细胞系具有优异的体外细胞毒性（IC50=0.8 μM），比阿霉素高 20 倍。通过 G2/M 期阻滞的细胞毒性作用似乎不是 ROS。
