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新型鬼臼毒素衍生物的合成及细胞毒性评价。

Synthesis and cytotoxicity evaluation of novel podophyllotoxin derivatives.

机构信息

Institute of Nautical Medicine, Nantong University, Nantong, P.R. China.

出版信息

Arch Pharm (Weinheim). 2011 Nov;344(11):735-40. doi: 10.1002/ardp.201100095. Epub 2011 Sep 2.

Abstract

Seven benzylamino derivatives of podophyllotoxin 8a-8g were synthesized and their chemical structures were confirmed by IR, ¹H-NMR, (13)C-NMR and ESI-MS spectral analyses. Their abilities to inhibit the growth of cancer cells A549, HCT-116 and HepG2, were investigated by MTT assay. Compound 8b possessed the highest cytotoxicity on cancer cell lines with average IC(50) values of 3.8 µM. All we synthetic compounds were cytotoxic against three cancer cell lines at the micromolar range, indicating podophyllotoxin derivatives with structural modification of benzylamino possess potent antitumor activity.

摘要

合成了 7 个鬼臼毒素 8a-8g 的苯甲氨基衍生物,并通过 IR、1H-NMR、(13)C-NMR 和 ESI-MS 光谱分析确认了它们的化学结构。通过 MTT 法测定了它们对肺癌细胞 A549、HCT-116 和 HepG2 生长的抑制能力。化合物 8b 对癌细胞系的细胞毒性最强,平均 IC50 值为 3.8μM。我们合成的所有化合物在微摩尔范围内对三种癌细胞系均具有细胞毒性,表明苯甲氨基结构修饰的鬼臼毒素衍生物具有潜在的抗肿瘤活性。

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