5435-28-9Relevant articles and documents
Synthesis of photocaged diamines and their application in photoinduced self-assembly
Barra, Tomas,Arrue, Lily,Urzúa, Esteban,Ratjen, Lars
, (2019/02/06)
The photochemical cleavage of covalent bonds is an important strategy in protection group chemistry, as well as for the triggering of chemical events posterior to the application of the physicochemical stimulus. Photocages allow the arresting and traceles
(Z)-1-Aryl-3-arylamino-2-propen-1-ones, highly active stimulators of tubulin polymerization: Synthesis, structure-activity relationship (SAR), tubulin polymerization, and cell growth inhibition studies
Reddy, M. V. Ramana,Akula, Balaiah,Cosenza, Stephen C.,Lee, Clement M.,Mallireddigari, Muralidhar R.,Pallela, Venkat R.,Subbaiah, D. R. C. Venkata,Udofa, Andrew,Reddy, E. Premkumar
experimental part, p. 5174 - 5187 (2012/08/28)
Tubulin, the major structural component of microtubules, is a target for the development of anticancer agents. A series of (Z)-1-aryl-3-arylamino-2- propen-1-one (10) were synthesized and evaluated for antiproliferative activity in cell-based assay. The most active compound (Z)-1-(2-bromo-3,4,5- trimethoxyphenyl)-3-(3-hydroxy-4-methoxyphenylamino)prop-2-en-1-one (10ae) was tested in 20 tumor cell lines including multidrug resistant phenotype and was found to induce apoptosis in all these cell lines with similar GI50 values. Flow cytometry studies showed that 10ae arrested the cells in G2/M phase of cell cycle. In addition to G2/M block, these compounds caused microtubule stabilization like paclitaxel and induced apoptosis via activation of the caspase family. The observations made in this investigation demonstrate that (Z)-1-Aryl-3-arylamino-2-propen-1-one (10) represents a new class of microtubule-stabilizing agents.
Concise syntheses of N-aryl-5,6,7-trimethoxyindoles as antimitotic and vascular disrupting agents: Application of the copper-mediated Ullmann-type arylation
Lee, Hsueh-Yun,Chang, Jang-Yang,Chang, Ling-Yin,Lai, Wen-Yang,Lai, Mei-Jung,Shih, Kuang-Hsing,Kuo, Ching-Chuan,Chang, Chi-Yen,Liou, Jing-Ping
, p. 3154 - 3157 (2011/05/12)
In an attempt to mimic the 3,4,5-trimethoxyphenyl-Z-stilbene moiety of combretastatin A-4, a series of N-aryl-5,6,7-trimethoxyindoles were synthesized via copper-catalyzed Ullmann-type N-arylation through the corresponding 5,6,7-trimethoxyindole and aryl halides. These synthesized compounds demonstrated potent antiproliferative activity providing a novel skeleton for potent tubulin polymerization inhibitors.
Z-stilbenes derivatives and the pharmaceutical composition thereof
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Page/Page column 4, (2008/06/13)
A series of Z-stilbenes derivatives are disclosed, which have the structure as shown by formula 1. In the structure of formula 1, X is hydrogen, NHR, or nitro group, and R is hydrogen. Y and Z is independently hydrogen, halogen, C1-C10 /s
2-Amino and 2′-aminocombretastatin derivatives as potent antimitotic agents
Chang, Jang-Yang,Yang, Ming-Fang,Chang, Chi-Yen,Chen, Chi-Ming,Kuo, Ching-Chuan,Liou, Jing-Ping
, p. 6412 - 6415 (2007/10/03)
A novel series of 2-amino and 2′-aminocombretastatin derivatives were synthesized and evaluated for antitumor activity. Several compounds had excellent antiproliferative activity as inhibitors of tubulin polymerization. Compounds 11, 20, and 21 with ICsu