多取代色酮衍生物的合成及抗增殖活性评价。
Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin Derivatives.
机构信息
China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Bioengineering, Tianjin University of Science and Technology, Tianjin 300457, China.
出版信息
Molecules. 2020 Dec 31;26(1):176. doi: 10.3390/molecules26010176.
A series of multi-substituted isatin derivatives were synthesized using the powerful Sandmeyer reaction. The structures of these derivatives were confirmed by H-NMR, C-NMR, and HR-MS. Inhibition of proliferation activities of these derivatives against human leukemia cells (K562), human hepatocellular carcinoma cells (HepG2) and human colon carcinoma cells (HT-29) were evaluated in vitro using the MTT assay. Among the series, compound exhibited strong antiproliferatory activities against K562, HepG2 and HT-29 cells with IC values of 1.75, 3.20, and 4.17 μM, respectively. The morphological, growth inhibitory and apoptosic effects of compound in K562 cells, wound healing effect in HepG2 cells, and tube formating effect in matrix gel of HUVEC cells were evaluated consequently. All results indicated that compound could be used as a potential antitumor agent in further investigations.
一系列多取代色胺衍生物通过强大的Sandmeyer 反应合成。这些衍生物的结构通过 H-NMR、C-NMR 和 HR-MS 得到确认。通过 MTT 法评估了这些衍生物对人白血病细胞（K562）、人肝癌细胞（HepG2）和人结肠癌细胞（HT-29）的体外增殖活性抑制作用。在该系列中，化合物 对 K562、HepG2 和 HT-29 细胞表现出强烈的增殖抑制活性，IC 值分别为 1.75、3.20 和 4.17 μM。随后评估了化合物 在 K562 细胞中的形态、生长抑制和凋亡作用、HepG2 细胞中的划痕愈合作用以及 HUVEC 细胞基质凝胶中的管状形成作用。所有结果表明，化合物 可作为进一步研究的潜在抗肿瘤剂。
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