13278-35-8Relevant articles and documents
Acridones circumvent P-glycoprotein-associated multidrug resistance (MDR) in cancer cells
Gopinath, Vadiraj S.,Thimmaiah, Padma,Thimmaiah, Kuntebommanahalli N.
, p. 474 - 487 (2008)
Multidrug resistance (MDR) mediated by overexpression of MDR1 P-glycoprotein (P-gp) is one of the best characterized transporter-mediated barriers to successful chemotherapy in cancer patients. Chemosensitizers are the agents that increase the sensitivity
Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia
Lewis, Timothy A.,Sykes, David B.,Law, Jason M.,Mu?oz, Benito,Rustiguel, Joane K.,Nonato, Maria Cristina,Scadden, David T.,Schreiber, Stuart L.
, p. 1112 - 1117 (2016)
Homeobox transcription factor A9 (HoxA9) is overexpressed in 70% of patients diagnosed with acute myeloid leukemia (AML), whereas only a small subset of AML patients respond to current differentiation therapies. A cell line overexpressing HoxA9 was derive
Potent acetylcholinesterase inhibitors: Design, synthesis, biological evaluation, and docking study of acridone linked to 1,2,3-triazole derivatives
Mohammadi-Khanaposhtani, Maryam,Saeedi, Mina,Zafarghandi, Narges Shamsaei,Mahdavi, Mohammad,Sabourian, Reyhaneh,Razkenari, Elahe Karimpour,Alinezhad, Heshmatollah,Khanavi, Mahnaz,Foroumadi, Alireza,Shafiee, Abbas,Akbarzadeh, Tahmineh
, p. 799 - 806 (2015)
A novel series of acridone linked to 1,2,3-triazole derivatives have been synthesized and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. The synthetic approach was started from the reaction of 2-bromobenzoic acid with aniline derivatives and subsequent cyclization reaction to give acridone derivatives. Then, reaction of the later compounds with propargyl bromide followed by azide-alkyne cycloaddition reaction (click reaction) led to the formation of the title compounds in good yields. Among the synthesized compounds, 10-((1-(4-chlorobenzyl)-1H-1,2,3-triazol-4-yl)methyl)-2-methoxyacridin-9(10H)-one 9g, depicted the most potent anti-AChE activity (IC50 Combining double low line 7.31 μ1/4M). Also, docking study confirmed the results obtained through in vitro experiments and predicted possible binding conformation.
Design, synthesis and bioactivity evaluation of novel N-phenyl-substituted evodiamine derivatives as potent anti-tumor agents
Hao, Xiangyong,Deng, Jiedan,Zhang, Honghua,Liang, Ziyi,Lei, Fang,Wang, Yuqing,Yang, Xiaoyan,Wang, Zhen
, (2022/01/10)
Natural products are important sources for the development of therapeutic medicine, among which evodia fruit has a wide range of medicinal properties in traditional Chinese medicine. Evodiamine, the main active component of evodia fruit, has various anti-cancer effects and has been proved to be a Topo inhibitor. From our previous attempts of modifying evodiamine, we found that the N14 phenyl substituted derivatives had showed great anti-tumor activity, which prompted us to further explore the novel structures and activities of these compounds. Compound 6f, as a N14 3-fluorinated phenyl substituted evodiamine derivative, showed a certain inhibitory activity against Topo I at 200 μM. By studying its anti-tumor effects in vitro, compound 6f could inhibit proliferation and induce apoptosis, as well as arrest the cell cycle of HGC-27 and HT-29 cell lines at G2/M phase in a concentration-dependent manner. Moreover, compound 6f could inhibit the migration and invasion of HGC-27 cell lines. Meanwhile, compound 6f could induce apoptosis of HGC-27 cells by inhibiting PI3K/AKT pathway. Overall, this work demonstrated that the N14 phenyl-substituted evodiamine derivatives had a good inhibitory effect on tumor cells in vitro, providing a promising strategy for developing potential anticancer agents for the treatment of gastrointestinal tumors.
COMPOUND FOR ORGANIC ELECTRONIC ELEMENT, ORGANIC ELECTRONIC ELEMENT USING THE SAME, AND AN ELECTRONIC DEVICE THEREOF
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Paragraph 0144; 0238; 0295-0298, (2020/10/31)
The present invention provides a compound represented by chemical formula 1, an organic electric device including a first electrode, a second electrode, and an organic material layer between the first electrode and the second electrode, and an electronic device including the organic electric device. By including the compound represented by chemical formula 1 in the organic material layer, the driving voltage of the organic electric device can be lowered, luminous efficiency and lifespan can be improved, and in particular, the lifespan can be improved.COPYRIGHT KIPO 2021
