17512-88-8Relevant articles and documents
Synthesis and anti-mitotic activity of 6,7-dihydro-4H-isothiazolo[4,5-b]pyridin-5-ones: In vivo and cell-based studies
Semenov, Victor V.,Lichitsky, Boris V.,Komogortsev, Andrey N.,Dudinov, Arkady A.,Krayushkin, Mikhail M.,Konyushkin, Leonid D.,Atamanenko, Olga P.,Karmanova, Irina B.,Strelenko, Yuri A.,Shor, Boris,Semenova, Marina N.,Kiselyov, Alex S.
, p. 573 - 585 (2016/10/12)
A series of 3,7-diaryl-6,7-dihydroisothiazolo [4,5-b]pyridin-5(4H)-ones 8 and 9 was synthesized by multicomponent condensation of 3-aryl-5-isothiazolecarboxylic acid esters 4a–f with aromatic (or thienyl) aldehydes 7 and Meldrum's acid in an acidic medium
Synthesis, characterization and anti-proliferation activities of novel cyano oximino sulfonate esters
El-Faham, Ayman,Elnakdy, Yasser Abbas,El Gazzar, Sarah Abdou Mohamed,El-Rahman, Mohamed Mokbel Abd,Khattab, Sherine Nabil
, p. 373 - 378 (2014/04/17)
A series of novel cyano oximino sulfonate derivatives were prepared from the reaction of arylsulfonyl chloride with different cyanoacetamide-based oximes ranging from the simplest unsubstituted amide to analogues containing N-ethyl (mimicking the Oxyma template), N-piperidinyl and N-morpholinyl chains. In addition, the cyano oximes, N-hydroxybenzimidoyl cyanide and N-hydroxypicolinimidoyl cyanide were also used in the synthesis of the novel cyano oximino sulfonate derivatives. The structures of the prepared compounds were confirmed by 1H-NMR, 13C-NMR, and elemental analysis. The preliminary bioassays showed that some of the title compounds, such as 2-oxo-2-(piperidin-1-yl)-N-(tosyloxy)acetimidoyl cyanide (TsPipOx), N-(tosyloxy)benzimidoyl cyanide (TsPhOX), N-(naphthalen-2-ylsulfonyloxy)-2-oxo- 2-(piperidin-1-yl)acetimidoyl cyanide (NpsPipOx), 2-amino-N-(naphthalen-2- ylsulfonyloxy)-2-oxoacetimidoyl cyanide (NpsAmOx), N-(naphthalen-2- ylsulfonyloxy)benzimidoyl cyanide (NpsPhCN), and N-(naphthalen-2-ylsulfonyloxy) picolinimidoyl cyanide (NpsPyCN), showed anti-proliferation effect on the mouse fibroblast L929. The calculated IC50-values were ranging between 36.5 μg/mL and 0.235 mg/mL. However the anti-proliferation effects seem to be cytostatic rather than cytotoxic. The compounds only minimize the growth activity without completely killing the cells.