85554-24-1Relevant articles and documents
Synthetic method of xanthene-9-formic acid
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Paragraph 0035; 0040; 0041; 0044; 0049; 0050, (2017/12/09)
The invention discloses a synthetic method of xanthene-9-formic acid, which belongs to the field of chemical synthesis. The method comprises the following steps: xanthone is taken as a raw material, then is reduced to xanthydrol under alkaline condition by zinc dust, then the xanthydrol is subjected to a halogenated reaction to obtain the halogenated xanthene, then under effect of a catalyst, a cyanidation reaction is generated to obtain 9-cyan xanthene, through alkali hydrolysis, organic impurity is removed through extraction of an organic solvent, a xanthene-9-formate aqueous solution is obtained, and a xanthene-9-formic acid product is obtained through a neutralization reaction. The method has the advantages of simple operation and safe technology, the xanthene-9-formic acid with high purity is obtained without refining, and the method is easy and effective for industrial production.
Selective serotonin receptor antagonists and therapeutic applications thereof
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Page 14-15, (2010/02/05)
Spiro[9,10-dihydroanthracene]-9,3′-pyrrolidine (SPAN) and derivatives thereof are provided as selective serotonin receptor antagonists. The compounds are selective, high affinity antagonists of 5-HT2 serotonin receptors. The compounds are useful as antidepressant and antianxiety agents.
New Triazine Derivatives as Potent Modulators of Multidrug Resistance
Dhainaut, Alain,Regnier, Gilbert,Atassi, Ghanem,Pierre, Alain,Leonce, Stephane,et al.
, p. 2481 - 2496 (2007/10/02)
A series of 70 triazine derivatives have been synthesized and tested for their capacity to modulate multidrug resistance (MDR) in DC-3F/AD and KB-A1 tumor cells in vitro, in comparison with verapamil (VRP), a calcium channel antagonist currently used in therapy as an antihypertensive drug, which also shows MDR modulating activity.Among the 12 selected compounds, 16 (S9788) showed high MDR reversing properties in vitro (300- and 6-fold VRP at 5μM in DC-3F/AD and KB-A1 cells, respectively) and induced a strong accumulation of adriamycin.The relationship between the increase of ADR accumulation and the fold reversal induced by these compounds and their lack of effects on the sensitive DC-3F cells suggest that they act mainly by inhibiting the P-glycoprotein (Pgp) catalyzed efflux of cytotoxic agents, as already described for a majority of MDR modulators.In vivo, in association with the antitumor drug vincristine (0.25 mg/kg), 16 (100 mg/kg) increased the T/C by 39percent in mice bearing the resistant tumor cell line P388/VCR.According to these interesting properties, 16 was selected for a clinical development because it is more bioavailable than 34, even though it was less active.