Abstract Two series of thiazinone and thiosemicarbazone derivatives (1-12) were synthesized using 2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-ones (ABNs) and 3–alkyl–2,6–diarylpiperidin–4–ones as the starting materials. The structures of newly synthesized compounds were established on the basis of FT–IR, NMR spectroscopy and mass spectrometry. From the spectroscopic data, we identified that the cyclization reaction of thioamide with dialkyl acetylenedicarboxylate selectively gives six membered methyl 2-(2-(2,4-disubstituted-3-azabicyclo[3.3.1]nonan-9-ylidene)hydrazinyl)-4-oxo-4H-1,3-thiazine-6-carboxylates (1-6). In order to investigate the antitumor activities of the synthesized compounds, in vitro cytotoxicity studies were carried out using human prostate cancer cell lines. Tested compounds showed good/moderate activities against cancer cell lines and further investigation carried out by live/dead assay. Graphical Abstract

中文翻译：

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一些新型噻嗪酮和缩氨基硫脲衍生物的合成、表征和抗肿瘤活性

摘要 使用 2,4-二芳基-3-氮杂双环[3.3.1]壬烷-9-酮 (ABNs) 和 3-烷基-2,6-二芳基哌啶-4 合成了两个系列的噻嗪酮和缩氨基硫脲衍生物 (1-12) ——作为起始材料。新合成化合物的结构是在红外光谱、核磁共振光谱和质谱的基础上建立的。从光谱数据中，我们确定硫代酰胺与乙炔二羧酸二烷基酯的环化反应选择性地得到六元甲基 2-(2-(2,4-二取代-3-氮杂双环 [3.3.1]nonan-9-ylidene)hydrazinyl)- 4-oxo-4H-1,3-thiazine-6-carboxylates (1-6)。为了研究合成化合物的抗肿瘤活性，使用人前列腺癌细胞系进行了体外细胞毒性研究。测试的化合物对癌细胞系显示出良好/中等的活性，并通过活/死测定进行了进一步研究。图形概要