- Novel anthraquinone compounds inhibit colon cancer cell proliferation via the reactive oxygen species/JNK pathway
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A series of amide anthraquinone derivatives, an important component of some traditional Chinese medicines, were structurally modified and the resulting antitumor activities were evaluated. The compounds showed potent anti-proliferative activities against eight human cancer cell lines, with no noticeable cytotoxicity towards normal cells. Among the candidate compounds, 1-nitro-2-acyl anthraquinone-leucine (8a) showed the greatest inhibition of HCT116 cell activity with an IC50 of 17.80 μg/mL. In addition, a correlation model was established in a three-dimensional quantitative structure-activity relationship (3D-QSAR) study using Comparative Molecular Field Analysis (CoMFA) and comparative molecular similarity index analysis (CoMSIA). Moreover, compound 8a effectively killed tumor cells by reactive oxygen species (ROS)-JNK activation, causing an increase in ROS levels, JNK phosphorylation, and mitochondrial stress. Cytochrome c was then released into cytoplasm, which, in turn activated the cysteine protease pathway and ultimately induced tumor cell apoptosis, suggesting a potential use of this compound for colon cancer treatment.
- Chen, Tinggui,Feng, Liheng,Guan, Yingying,Guo, Fang,Li, Yuying,Liu, Yaoming,Ma, Kaiqing,Su, Qiang,Wang, Zhuanhua,Zhang, Liwei,Zhou, Yuzhi
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- Synthesis of linear and angular anthraquinonoisothiazol-3-ones, their S-oxides, and S,S-dioxides
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2-Methyltetrahydroanthra[2,3-d]isothiazole-3,5,10-trione and 2-R-tetrahydroanthra[2,1-d]isothiazole-3,6,11-triones were synthesized by the reactions of 3-chloro-9,10-dioxo-9,10-dihydroanthracene-2-carboxamide and 1-nitro-9,10-dioxo-9,10-dihydroanthracene-
- Kucherov,Zlotin
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p. 1657 - 1662
(2007/10/03)
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