Synthesis of Novel Pyrido[4,3-e][1,2,4]triazino[3,2-c][1,2,4]thiadiazine 6,6-dioxide Derivatives with Potential Anticancer Activity

Molecules

Jarosᐪw Sᐪwiński¹  Aleksandra Grzonek¹  Beata Żołnowska¹  Anna Kawiak² 

[1] Department of Organic Chemistry, Medical University of Gdańsk, Al. Gen. J. Hallera 107, 80-416 Gdańsk, Poland;Department of Biotechnology, Intercollegiate Faculty of Biotechnology, University of Gdańsk and Medical University of Gdańsk, Ul. Kładki 24, 80-822 Gdańsk, Poland;

关键词: pyrido[4;    3-e][1;    2;    4]triazino[3;    2-c][1;    2;    4]thiadiazine;    6;    6-dioxides;    synthesis;    NMR studies;    cytotoxic activity;   

DOI  :  10.3390/molecules21010041

来源: mdpi

【 摘 要 】

A series of novel 3-/2,3-substituted pyrido[4,3-e][1,2,4]triazino[3,2-c][1,2,4]thiadiazine 6,6-dioxides 4–28 have been synthesized by the reaction of 3-amino-2-(4-thioxo-1,4-dihydropyridin-3-yl-sulfonyl)guanidine with either 2-oxoalkanoic acids and its esters, or phenylglyoxylic hydrates in glacial acetic acid. Some of them exhibited reasonable or moderate anticancer activity toward human cancer cell lines, HCT-116, MCF-7 and HeLa. The structure of this novel heterocyclic ring system was confirmed by ¹D-NMR and ²D-NMR spectroscopic data including COSY, ROESY and HMBC, elemental analyses and MS spectrometry.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.