title: 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.
abstract: 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.
authors.affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Al. Gen. J. Hallera 107, 80-416 Gdańsk, Poland. jaroslaw@gumed.edu.pl.
authors.forename: Jarosław
authors.initials: J
authors.lastname: Sławiński
authors.affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Al. Gen. J. Hallera 107, 80-416 Gdańsk, Poland. aleksandra@gumed.edu.pl.
authors.forename: Aleksandra
authors.initials: A
authors.lastname: Grzonek
authors.affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Al. Gen. J. Hallera 107, 80-416 Gdańsk, Poland. zolnowska@gumed.edu.pl.
authors.forename: Beata
authors.initials: B
authors.lastname: Żołnowska
authors.affiliation: Department of Biotechnology, Intercollegiate Faculty of Biotechnology, University of Gdańsk and Medical University of Gdańsk, Ul. Kładki 24, 80-822 Gdańsk, Poland. kawiak@biotech.ug.edu.pl.|Department of Human Physiology, Medical University of Gdańsk, Ul. Tuwima 15, 80-210 Gdańsk, Poland. kawiak@biotech.ug.edu.pl.
authors.forename: Anna
authors.initials: A
authors.lastname: Kawiak
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D045325:HCT116 Cells; D006367:HeLa Cells; D006577:Heterocyclic Oxides / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D061986:MCF-7 Cells; D013329:Structure-Activity Relationship; D013829:Thiadiazines / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D006577:Heterocyclic Oxides; D013829:Thiadiazines
keywords: 6,6-dioxides; NMR studies; cytotoxic activity; pyrido[4,3-e][1,2,4]triazino[3,2-c][1,2,4]thiadiazine; synthesis