848357-27-7Relevant academic research and scientific papers
Diaryl-substituted 1, 1-ethylene compounds and preparation method and application thereof
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Paragraph 0049-0051, (2021/02/24)
The invention discloses diaryl-substituted 1, 1-ethylene compounds shown as general formulas I, II, III and IV, and a preparation method and application thereof, and the compounds can be used for preparing medicines related to tumor treatment, tubulin activity inhibition and HDAC activity inhibition.
Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site
Li, Wenlong,Shuai, Wen,Sun, Honghao,Xu, Feijie,Bi, Yi,Xu, Jinyi,Ma, Cong,Yao, Hequan,Zhu, Zheying,Xu, Shengtao
, p. 428 - 442 (2018/12/13)
A series of novel isocombretastatin A-4 (isoCA-4) analogs were designed and synthesized by replacing 3,4,5-trimethoylphenyl and isovanillin of isoCA-4 with quinoline and indole moieties, respectively. The structure activity relationships (SARs) of these synthesized quinoline-indole derivatives have been intensively investigated. Two compounds 27c and 34b exhibited the most potent activities against five cancer cell lines with IC50 values ranging from 2 to 11 nM, which were comparable to those of Combretastatin A-4 (CA-4, 1). Further mechanism investigations revealed that 34b effectively inhibited the microtubule polymerization by binding to the colchicine site of tubulin. Further cellular mechanism studies elucidated that 34b disrupted cell microtubule networks, arrested the cell cycle at G2/M phase, induced apoptosis and depolarized mitochondria of K562 cells. Moreover, 34b displayed potent anti-vascular activity in both wound healing and tube formation assays. Importantly, 27c and 34b significantly inhibited tumor growth in H22 xenograft models without apparent toxicity, suggesting that 27c and 34b deserve further research as potent antitumor agents for cancer therapy.
THIENOPYRAZOLES
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Page/Page column 73-74, (2008/06/13)
Thienopyrazoles, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical uses in the treatment of disease states capable of being modulated by the inhibition of the protein kinases, in particular interleukin-2 inducible tyrosine kinase (ITK).
