The synthesis of a small library of 8-substituted 2-methyl-5,6,7,8-tetrahydroquinoline derivatives is presented. All the compounds were tested for their antiproliferative activity in non-cancer human dermal microvascular endothelial cells (HMEC-1) and cancer cells: human T-lymphocyte cells (CEM), human cervix carcinoma cells (HeLa), human dermal microvascular endothelial cells (HMEC-1), colorectal adenocarcinoma (HT-29), ovarian carcinoma (A2780), and biphasic mesothelioma (MSTO-211H). Compounds 3a, 5a, and 2b, showing significant IC50 values against the whole panel of the selected cells, were further synthesized and tested as pure enantiomers in order to shed light on how their stereochemistry might impact on the related biological effect. The most active compound (R)-5a was able to affect cell cycle phases and to induce mitochondrial membrane depolarization and cellular ROS production in A2780 cells.

中文翻译：

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新型手性2-甲基-5,6,7,8-四氢喹啉-8-胺类化合物的生物学特性

介绍了 8-取代 2-甲基-5,6,7,8-四氢喹啉衍生物的小型库的合成。测试了所有化合物在非癌人类真皮微血管内皮细胞 (HMEC-1) 和癌细胞中的抗增殖活性：人类 T 淋巴细胞 (CEM)、人类子宫颈癌细胞 (HeLa)、人类真皮微血管内皮细胞 ( HMEC-1)、结直肠腺癌 (HT-29)、卵巢癌 (A2780) 和双相间皮瘤 (MSTO-211H)。化合物 3a、5a 和 2b 对整个选定细胞组显示出显着的 IC50 值，它们被进一步合成并作为纯对映异构体进行测试，以阐明它们的立体化学可能如何影响相关的生物效应。