- Synthesis of N-Carbonyl Acridanes as Highly Potent Inhibitors of Tubulin Polymerization via One-Pot Copper-Catalyzed Dual Arylation of Nitriles with Cyclic Diphenyl Iodoniums
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A novel Copper-catalyzed cascade reaction between six-membered cyclic diaryliodonium salts and nitriles is reported for the facile access to a variety of N-carbonyl acridanes in good to excellent yields (up to 82%). The reaction is efficient and atom-economical with a broad substrate scope (e. g. both aryl / alkyl nitriles and substituted / unsubstituted cyclic diaryliodonium salts compatible in the system). This method is particularly useful for the synthesis of substituted N-carbonyl acridanes which are present in many pharmaceutically important compounds, but are not easy to obtain in conventional approaches. Furthermore, one of the newly synthesized acridanes displayed high antiproliferative activity against MB-468 cancer cells (IC50=26 nM, comparable to paclitaxel and colchicine) by inhibiting tubulin polymerization. Together, these findings might grant a rapid access to a novel molecular scaffold with potential anticancer utilities. (Figure presented.).
- Peng, Xiaopeng,Li, Ling,Ren, Yichang,Xue, Huanxin,Liu, Jin,Wen, Shijun,Chen, Jianjun
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supporting information
p. 2030 - 2038
(2020/04/15)
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- N-carbonyl-9,10-dihydroacridine compound and applications thereof
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The invention relates to an N-carbonyl-9,10-dihydroacridine compound, wherein the structural formula of the compound is represented by the following formula (I), and R is alkoxy substituted phenyl,ether substituted phenyl, cyclohexane or cyclopropane. The N-carbonyl-9,10-dihydroacridine compound provided by the invention has remarkable inhibition effect on tumor cells, and can be used for preparing anti-cancer drugs.
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Paragraph 0019-0024
(2020/05/01)
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