Doctoral School of The Medical University of Silesia, 40-055 Katowice, Poland.
Department of Organic Chemistry, Faculty of Pharmaceutical Sciences, The Medical University of Silesia, Jagiellońska 4, 41-200 Sosnowiec, Poland.
Molecules. 2023 Nov 19;28(22):7662. doi: 10.3390/molecules28227662.
Many new isomeric dipyridothiazine dimers have been presented as molecules with anticancer potential. These compounds were obtained in efficient syntheses of 1,6-, 1,8-, 2,7- and 3,6-diazaphenothiazines with selected alkylaromatic linkers. The structures of these compounds has been proven with two-dimensional spectroscopic techniques (COSY, NOESY, HSQC and HMBC) and high-resolution mass spectrometry (HRMS). In silico analyses of probable molecular targets were performed using the Way2Drug server. All new dimers were tested for anticancer activity against breast cancer line MCF7 and colon cancer line SW480. Cytotoxicity was assessed on normal L6 muscle cells. The tested dimers had high anticancer potential expressed as IC and the selectivity index SI. The most active derivative, , showed an IC activity of less than 1 µM and an SI selectivity index higher than 100. Moreover, the compounds were characterized by low toxicity towards normal cells, simultaneously indicating a high cytostatic potential.
许多新的二吡啶并噻嗪二聚体被呈现为具有抗癌潜力的分子。这些化合物是通过高效合成 1,6-、1,8-、2,7-和 3,6-二氮杂苯并噻嗪与选定的芳基烷基连接体获得的。这些化合物的结构已通过二维光谱技术（COSY、NOESY、HSQC 和 HMBC）和高分辨率质谱（HRMS）得到证实。使用 Way2Drug 服务器对可能的分子靶标进行了计算机分析。所有新的二聚体都针对乳腺癌细胞系 MCF7 和结肠癌细胞系 SW480 进行了抗癌活性测试。细胞毒性在正常 L6 肌肉细胞上进行评估。测试的二聚体表现出高的抗癌活性，IC 表示低至 1µM 和选择性指数 SI 高于 100。此外，这些化合物对正常细胞的毒性低，同时表明具有高的细胞抑制潜力。
