22315-94-2Relevant academic research and scientific papers
New benzoxanthone derivatives as topoisomerase inhibitors and DNA cross-linkers
Cho, Hee-Ju,Jung, Mi-Ja,Woo, Sangwook,Kim, Jungsook,Lee, Eung-Seok,Kwon, Youngjoo,Na, Younghwa
, p. 1010 - 1017 (2010)
We synthesized 12 benzoxanthone derivatives classified as three different groups based on the tetracyclic ring shapes and evaluated their pharmacological activities to find potential anticancer agents. In the cytotoxicity test, most compounds showed effective cancer cell growth inhibition against the HT29 and DU145 cell lines. Among the compounds tested, compound 19 was the most effective in the cancer cell lines tested. Compound 9 showed dual inhibitory activities against DNA relaxation by topoisomerases I and II. The% inhibition of compound 9 on topoisomerase I was comparable to that of camptothecin. Compound 9 efficiently blocked topoisomerase II function by almost threefold than etoposide at 20 μM. Compound 19 had selective topoisomerase II inhibitory activity at 100 μM. The DNA cross-linking test revealed that only compounds 8 and 19, which possess epoxy groups, cross-linked DNA duplex, while 14 did not. From the combined pharmacological results, we proposed that the target through which compound 19 inhibits cancer cell growth may be the DNA duplex itself and/or DNA-topoisomerase II complex.
Synthesis of xanthone derivatives with extended π-systems as α-glucosidase inhibitors: Insight into the probable binding mode
Liu, Yan,Ma, Lin,Chen, Wen-Hua,Wang, Bo,Xu, Zun-Le
, p. 2810 - 2814 (2007)
A series of novel xanthone derivatives with extended π-systems, that is, benzoxanthones 2-4, and their structurally perturbed analogs 5-9 have been designed and synthesized as α-glucosidase inhibitors. Their inhibitory activities toward yeast's α-glucosidase were evaluated with the aim to enrich the structure-activity relationship. The results indicated that benzoxanthones 2-4 were capable of inhibiting in vitro yeast's α-glucosidase 17- to 28-fold more strongly than xanthone derivative 1 that has smaller conjugated π-system. Benzoxanthone 8, bearing angularly fused aromatic rings, and reduced benzoxanthone 5 showed decreased activities, strongly suggesting that linearly conjugated π-systems play a crucial role in the inhibition process. O-Methylation of 3-OH of benzoxanthone 2 and nitration at C4 position led to a large decrease in the activity. This indicates that 3-OH of benzoxanthone was crucial to the inhibitory activity, primarily as an H-bonding donor. The present results suggest that π-π stacking effect and H-bonding make substantial contributions to elicit the inhibitory activities of this general class of inhibitors.
Synthesis and biological evaluation of novel benzo[b]xanthone derivatives as potential antitumor agents
Luo, Lin,Qin, Jiang-Ke,Dai, Zhi-Kai,Gao, Shi-Hua
, p. 1301 - 1308 (2013)
Nine novel aminoalkoxy substituted benzo[b]xanthones (3a-i) were synthesized. Their antitumor activities were evaluated in five human solid tumor cell lines, including Hep-G2, BEL-7402, HeLa, MGC-803 and CNE, by the MTT (2-(4,5-dimethyl-thiazol-2-yl)-3,5-
Synthesis and cytotoxic activity of benzopyranoxanthone analogues of benzo[b]acronycine and psorospermine
Sittisombut, Chavalit,Costes, Nadine,Michel, Sylvie,Koch, Michel,Tillequin, Francois,Pfeiffer, Bruno,Renard, Pierre,Pierre, Alain,Atassi, Ghanem
, p. 675 - 679 (2001)
Condensation of 3-hydroxy-2-naphthalenecarboxylic acid with phloroglucinol afforded 1,3-dihydroxy-12H-benzo[b]xanthen-12-one. Construction of an additional dimethylpyran ring onto this skeleton, by alkylation with 3-chloro-3-methyl-1-butyne followed by Claisen rearrangement, gave access to a series of benzo[b]pyrano[2,3-i]xanthen-6-ones and benzo[b]pyrano[3,2-h]xanthen-7-ones related to psorospermine and benzo[b]acronycine. In contrast with what is observed in the pyridoacridone and benzopyridoacridone series, the linear benzo[b]-pyrano[2,3-i]xanthen-6-one derivatives were more potent than their angular benzo[b]pyrano[3,2-h]xanthen-7-one isomers. cis-3,4-Diacetoxy-5-methoxy-2,2-dimethyl-3,4-dihydro-2H,6H-benzo[b]pyrano [2,3,i]xanthen-6-one, the most active among the new compounds, was more potent than acronycine in inhibiting the proliferation of L1210 murine leukemia cells.
* One derivative containing nitrogen and its preparation method and application (by machine translation)
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Paragraph 0162-0164, (2017/01/31)
The invention discloses a formula (I) of formula (II) containing nitrogen mouth Shan Tong derivative and its preparation method and application, A new synthesis of this invention containing nitrogen mouth Shan Tong derivatives of the salt and its acid salt, increased solubility, active research indicates part of the compound at the same time with treating and/or preventing diabetes and complications from diabetes mellitus the role of the, can further carry out development research as a model for treating and/or preventing diabetes caused by the complications of diabetes medicine. (by machine translation)
NOVEL ANTICANCER-AIDING COMPOUND, METHOD FOR PREPARING THE SAME, ANTICANCER-AIDING COMPOSITION CONTAINING THE SAME AND METHOD FOR REDUCING ANTICANCER DRUG RESISTANCE USING THE SAME
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Page/Page column 13, (2012/07/31)
The present invention provides a novel xanthone derivative compound or a pharmaceutically acceptable salt thereof. The compound is useful as a chemosensitizer that reduces anticancer drug resistance.
