Tetrahedron ( IF 2.1 ) Pub Date : 2021-09-21 , DOI: 10.1016/j.tet.2021.132454 Baolong Hou 1 , Ying Zhou 1 , Wenyu Li 1 , Jianli Liu 1 , Cuiling Wang 1
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Here, an efficient and convenient method has been developed for the rapid preparation of N-substituted tryptanthrin analogues through the reaction of tryptanthrins and secondary amines under mild reaction conditions. All compounds were tested for their anti-tumor activity in cancer cell lines by MTT assay. The results showed that some of them exhibited anti-tumor activity against human tumor cell lines A549, HCT116, MDA-MB-231 with IC50 mean values at a low micromolar level. In particular, compound 3b induced G2/S cell cycle arrest and apoptosis in A549 cells dose-dependently.
中文翻译：
抗肿瘤剂色氨酸的合成与评价
在这里，通过色氨酸和仲胺在温和的反应条件下反应快速制备 N-取代的色氨酸类似物，开发了一种有效和方便的方法。通过MTT测定法测试所有化合物在癌细胞系中的抗肿瘤活性。结果表明，其中一些对人肿瘤细胞系 A549、HCT116、MDA-MB-231 表现出抗肿瘤活性，IC 50平均值处于低微摩尔水平。具体而言，化合物3b剂量依赖性地诱导A549细胞中的G2/S细胞周期停滞和细胞凋亡。
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