3,6-二溴咔唑和 5-溴吲哚衍生物的合成、抗癌和抗迁移评估。
Synthesis, Anti-Cancer and Anti-Migratory Evaluation of 3,6-Dibromocarbazole and 5-Bromoindole Derivatives.
机构信息
Department of Pharmaceutical Sciences, University of Puerto Rico, School of Pharmacy, San Juan 00936, Puerto Rico.
Department of Biology, College of Natural Sciences, University of Puerto Rico, San Juan 00931, Puerto Rico.
出版信息
Molecules. 2019 Jul 24;24(15):2686. doi: 10.3390/molecules24152686.
In this study, a new series of -alkyl-3,6-dibromocarbazole and -alkyl-5-bromoindole derivatives have been synthesized and evaluated in vitro as anti-cancer and anti-migration agents. Cytotoxic and anti-migratory effects of these compounds were evaluated in MCF-7 and MDA-MB-231 breast cancer cell lines and an insight on the structure-activity relationship was developed. Preliminary investigations of their anti-cancer activity demonstrated that several compounds have moderate antiproliferative effects on cancer cell lines with GI values in the range of 4.7-32.2 µM. Moreover, carbazole derivatives , , , , and inhibit migration activity of metastatic cell line MDA-MB-231 in the range of 18-20%. The effect of compounds , , and in extension of invadopodia and filopodia was evaluated by fluorescence microscopy and results demonstrated a reduction in actin-based cell extensions by compounds and .
在这项研究中，我们合成了一系列新的 - 烷基 -3,6- 二溴咔唑和 - 烷基 -5- 溴吲哚衍生物，并将其作为抗癌和抗迁移剂进行了体外评估。我们评估了这些化合物对 MCF-7 和 MDA-MB-231 乳腺癌细胞系的细胞毒性和抗迁移作用，并对其构效关系进行了研究。初步的抗癌活性研究表明，几种化合物对癌细胞系具有中等的增殖抑制作用，GI 值在 4.7-32.2µM 范围内。此外，咔唑衍生物 、 、 、 、 和 抑制转移性细胞系 MDA-MB-231 的迁移活性，范围为 18-20%。通过荧光显微镜评估了化合物 、 、 和 对延伸的侵袭伪足和丝状伪足的影响，结果表明化合物 和 减少了基于肌动蛋白的细胞延伸。
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