齐墩果酸作为开发新型抗肿瘤化合物的三萜模板。
Hederagenin as a triterpene template for the development of new antitumor compounds.
机构信息
Department of Chemistry, Universidade Federal de Viçosa, Av. P. H. Rolfs, s/n, CEP 36570-900, Viçosa, MG, Brazil; Department of Chemistry, Universidade Federal de Minas Gerais, Av. Pres. Antônio Carlos 6627, Campus Pampulha, CEP 31270-901, Belo Horizonte, MG, Brazil.
Department of Chemistry, Universidade Federal de Viçosa, Av. P. H. Rolfs, s/n, CEP 36570-900, Viçosa, MG, Brazil.
出版信息
Eur J Med Chem. 2015 Nov 13;105:57-62. doi: 10.1016/j.ejmech.2015.10.006. Epub 2015 Oct 9.
In this study, a series of novel C-28 esters and amides derivatives of hederagenin (He) were designed and synthesized in attempt to develop potent antitumor agents. Their structures were confirmed by MS, IR, (1)H NMR and (13)C NMR spectroscopic analyses and their cytotoxic activities were screened in SRB assays using a panel of six human cancer cell lines. Although most of the compounds displayed moderate to high levels of cytotoxic activity they were all more potent than the natural product He. The most active compounds had either an ethylpyrimidinyl (27) or an ethylpyrrolidinyl (28) substituent, with EC50 in the range of 1.1-6.5 μM for six human cancer cell lines. Notably, this corresponds to an approximately 30-fold times greater potency than He.
在这项研究中，设计并合成了一系列新型的羽扇豆烷（He）的 C-28 酯和酰胺衍生物，试图开发有效的抗肿瘤药物。通过 MS、IR、（1）H NMR 和（13）C NMR 光谱分析确认了它们的结构，并使用一组六种人癌细胞系在 SRB 测定中筛选了它们的细胞毒性活性。尽管大多数化合物表现出中等至高强度的细胞毒性活性，但它们都比天然产物 He 更有效。最活性的化合物具有乙基嘧啶基（27）或乙基吡咯烷基（28）取代基，对六种人癌细胞系的 EC50 范围在 1.1-6.5 μM 之间。值得注意的是，这相当于 He 的大约 30 倍的效力。
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