Synthesis and anti-mitotic activity of 6,7-dihydro-4H-isothiazolo[4,5-b]pyridin-5-ones: In vivo and cell-based studies

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• 作者：Victor V. Semenov^a ; ^{vs@zelinsky.ru} ; Boris V. Lichitsky^a ; ^{blich2006@mail.ru} ; Andrey N. Komogortsev^a ; ^dna5@mail.ru ; Arkady A. Dudinov^a ; ^{1944ark@mail.ru} ; Mikhail M. Krayushkin^a ; ^{mkray@ioc.ac.ru} ; Leonid D. Konyushkin^a ; ^{LeonidK@chemical-block.com} ; Olga P. Atamanenko^a ; ^{info@chemblock.com} ; Irina B. Karmanova^a ; ^{vs@chemblock.ru} ; Yuri A. Strelenko^a ; ^{strel@ioc.ac.ru} ; Boris Shor^b ; ^{boris.shor@immunepharma.com} ; Marina N. Semenova^c ; ^d ; ^{ms@chemical-block.com} ; Alex S. Kiselyov^e ; ^{nikizalp@aol.com}
• 关键词：Isothiazoles ; Dihydroisothiazolopyridinones ; Microtubule destabilization ; Sea urchin embryo ; Cytotoxicity
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：573-585
• 全文大小：2706 K
• 卷排序：125

文摘

Synthesis of dihydroisothiazolopyridinones (DIP). Antimitotic antitubulin activity of DIP in the sea urchin embryo model. Cytotoxicity of DIP against human cancer cell lines. Cell cycle arrest and cellular microtubule disruption. Microtubule destabilizing mode of action of DIP.