喜树碱-4β-三唑基-鬼臼毒素缀合物的合成及抗肿瘤活性。
Synthesis and antitumor activity of camptothecin- 4β-triazolopodophyllotoxin conjugates.
机构信息
Key Laboratory of Pu-er Tea Science, Ministry of Education, College of Science, Yunnan Agricultural University, Kunming, China.
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, China.
出版信息
Nat Prod Res. 2020 Aug;34(16):2301-2309. doi: 10.1080/14786419.2018.1538223. Epub 2019 Jan 12.
Two new compounds ( and ) having a camptothecin (CPT) analog conjugated to the 4β-azido-4-deoxypodophyllotixin analog by untilizing the copper-catalyzed azide-alkyne cycloadditon (CuAAC) reaction, and were evaluated for their cytotoxicity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using the MTT (3-(4,5-dimethyl-thiahiazo-2-yl)-2,5-diphenyltetrazolium bromide) assay. Two novel conjugates shown weak cytotoxicity, compound showed highly potent against HL-60 cell line tested, with IC value 17.69 ± 0.19 μM. This compound suggested its potential as anticancer agents for further development. [Formula: see text].
两个新的化合物（和）通过利用铜催化的叠氮-炔环加成（CuAAC）反应，将喜树碱（CPT）类似物连接到 4β-叠氮-4-去氧鬼臼毒素类似物上，并用 MTT（3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四唑溴盐）测定法评估了它们对五种人癌细胞系（HL-60、SMMC-7721、A-549、MCF-7 和 SW480）的细胞毒性。两种新型缀合物显示出较弱的细胞毒性，化合物对测试的 HL-60 细胞系表现出高活性，IC 值为 17.69 ± 0.19 μM。该化合物表明其具有进一步开发为抗癌药物的潜力。[化学式：见正文]。
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