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.
Highlights
Cancer is the second most life threatening non-communicable disease after cardiovascular disease, according to the World Health Organization [1]
It is known that 2-alkylthio-5-chloro-N-(1,2,4-triazin-yl)benzenesulfonamides V exhibit anticancer activity against colon, CNS, melanoma, ovarian, breast, renal, and leukemia cell lines [4]
We have developed of a new method for the synthesis investigate anticancer activity of arylsulfonamides modified by pyridothiadiazine and 1,2,4-triazine of 2,3-diaryl-9,9-dioxo-1H-9-thia-1,4,4a,7,10-pentaazaphenanthrene-2-ols
Summary
Cancer is the second most life threatening non-communicable disease after cardiovascular disease, according to the World Health Organization [1]. Despite the availability of numerous anticancer drugs, cancer is still hard to cure, especially without exhibiting any side effects. Heterocyclic scaffolds play an important role for the design of novel drugs by enhancing their biological effects when fused with other ring systems. It is known that 2-alkylthio-5-chloro-N-(1,2,4-triazin-yl)benzenesulfonamides V exhibit anticancer activity against colon, CNS, melanoma, ovarian, breast, renal, and leukemia cell lines [4]. Other analogs of 6-azauridine, the S-alkyl derivatives of 1,2,4-triazinone VII, present cytotoxic activities against human breast cancer (MCF-7), colon carcinoma (HCT-116) and hepatocellular carcinoma (Hep-G2) cell lines [6]. Tirapazamine VIII is a known bioreductive hypoxia-selective cytotoxin, currently undergoing a variety of phase I, II and III clinical trials for the treatment of various human cancers, including non-small cell lung, cervical, head
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