DISFARM, Sezione di Chimica Generale e Organica "A. Marchesini", Università degli Studi di Milano via Venezian, 21, 20133 Milano, Italy.
Dipartimento di Scienze del Farmaco, Università degli Studi di Padova, via F. Marzolo, 5, 35131 Padova, Italy.
Molecules. 2020 Nov 27;25(23):5561. doi: 10.3390/molecules25235561.
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 , , and , showing significant IC 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 was able to affect cell cycle phases and to induce mitochondrial membrane depolarization and cellular ROS production in A2780 cells.
本文介绍了 8-取代 2-甲基-5,6,7,8-四氢喹啉衍生物的小库合成。所有化合物均在非癌人类真皮微血管内皮细胞（HMEC-1）和癌细胞中进行了抗增殖活性测试：人 T 淋巴细胞（CEM）、人宫颈癌细胞（HeLa）、人真皮微血管内皮细胞（HMEC-1）、结肠直肠腺癌（HT-29）、卵巢癌细胞（A2780）和双相间皮瘤（MSTO-211H）。化合物 、 、 和 对所选细胞的整个细胞系表现出显著的 IC 值，进一步合成并作为纯对映异构体进行测试，以阐明其立体化学如何影响相关的生物学效应。最活性化合物 能够影响 A2780 细胞的细胞周期阶段，并诱导线粒体膜去极化和细胞 ROS 产生。
