100334-95-0Relevant articles and documents
Synthesis of xanthone derivatives and studies on the inhibition against cancer cells growth and synergistic combinations of them
Liu, Jie,Zhang, Jianrun,Wang, Huailing,Liu, Zhijun,Zhang, Cao,Jiang, Zhenlei,Chen, Heru
, p. 50 - 61 (2017)
34 Xanthones were synthesized by microwave assisted technique. Their in?vitro inhibition activities against five cell lines growth were evaluated. The SAR has been thoroughly discussed. 7-Bromo-1,3-dihydroxy-9H-xanthen-9-one (3-1) was confirmed as the most active agent against MDA-MB-231?cell line growth with an IC50 of 0.46?±?0.03?μM. Combination of 3-1 and 5,6-dimethylxanthone-4-acetic acid (DMXAA) showed the best synergistic effect. Apoptosis analysis indicated different contributions of early/late apoptosis and necrosis to cell death for both monomers and the combination. Western Blot implied that the combination regulated p53/MDM2 to a better healthy state. Furthermore, 3-1 and DMXAA arrested more cells on G2/M phase; while the combination arrested more cells on S phase. All the evidences support that the 3-1/DMXAA combination is a better anti-cancer therapy.
Incorporation of nitric oxide donor into 1,3-dioxyxanthones leads to synergistic anticancer activity
Liu, Jie,Zhang, Cao,Wang, Huailing,Zhang, Lei,Jiang, Zhenlei,Zhang, Jianrun,Liu, Zhijun,Chen, Heru
, p. 158 - 172 (2018)
Fifty 1,3-dioxyxanthone nitrates (4a ~ i-n, n = 1–6) were designed and synthesized based on molecular similarity strategy. Incorporation of nitrate into 1,3-dioxyxanthones with electron-donating groups at 6–8 position brought about synergistic anticancer effect. Among them, compound 4g-4 was confirmed the most active agent against HepG-2 cells growth with an IC50 of 0.33 ± 0.06 μM. It dose-dependently increased intramolecular NO levels. This activity was attenuated by either NO scavenger PTIO or mitochondrial aldehyde dehydrogenase (mtADH) inhibitor PCDA. Apoptosis analysis indicated different contributions of early/late apoptosis and necrosis to cell death for different dose of 4g-4. 4g-4 arrested more cells on S phase. Results from Western Blot implied that 4g-4 regulated p53/MDM2 to promote cancer cell apoptosis. All the evidences support that 4g-4 is a promising anti-cancer agent.
Donor compound as Xanthone-NO well as preparation method and application thereof in preparation of anti-tumor drugs (by machine translation)
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Page/Page column 5; 6; 12-14, (2020/01/04)
The invention belongs to the technical field of, antitumor drugs, and Xanthone - NO discloses a compound of formula I as well as a preparation method thereof, and an Xanthone - NO. application according to the: invention in preparation of an antitumor drug. In-flight vehicle, R1 , R2 , R3 The compound of the present invention is H, OH, Cl, Br prepared F;n=2-8. from substituted salicylic acid and m-taminophen and then is prepared xanthones, from the 1,n - substituted salicylic acid and the 3 - O - M xanthone,bromophenol to. prepare the compound of the, present invention for inhibiting the tumor cell proliferation in vitro and, inhibiting the apoptosis of tumor cells by multiple, targets. (by machine translation)