491-64-5Relevant articles and documents
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; 8; 9, (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)
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 (2018/04/05)
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.
Anti-AIDS agents 85. Design, synthesis, and evaluation of 1R,2R-dicamphanoyl-3,3-dimethyldihydropyrano-[2,3-c]xanthen-7(1H)-one (DCX) derivatives as novel anti-HIV agents
Zhou, Ting,Shi, Qian,Chen, Chin-Ho,Huang, Li,Ho, Phong,Morris-Natschke, Susan L.,Lee, Kuo-Hsiung
experimental part, p. 86 - 96 (2012/03/08)
In this study, 1R,2R-dicamphanoyl-3,3-dimethydihydropyrano[2,3-c]xanthen- 7(1H)-one (DCX) derivatives were designed and synthesized as novel anti-HIV agents against both wild-type and non-nucleoside reverse transcriptase (RT) inhibitor-resistant HIV-1 (RTMDR-1) strains. Twenty-four DCX analogs (6-29) were synthesized and evaluated against the non-drug-resistant HIV-1 NL4-3 strain, and selected analogs were also screened for their ability to inhibit the RTMDR-1 strain. Compared with the control 2-ethyl-3′,4′-di-O-(-)- camphanoyl-2′,2′-dimethyldihydropyrano[2,3-f]chromone (2-EDCP, 2), one of the best anti-HIV coumarin derivatives in our prior study, three DCX compounds (7, 12, and 22) showed better activity against both HIV strains with an EC50 range of 0.062-0.081 μM, and five additional compounds (8, 11, 16, 18, and 21) exhibited comparable anti-HIV potency. Six DCX analogs (7, 11-12, 18, and 21-22) also showed enhanced selectivity index (SI) values in comparison to the control. Structure-activity relationship (SAR) information suggested that the extended conjugated system of the pyranoxanthone skeleton facilitates the interaction of the small DCX molecule within the viral binding pocket, consequently leading to enhanced anti-HIV activity and selectivity. Compared to DCP compounds, DCX analogs are a more promising new class of anti-HIV agents.