多环芳烃衍生的β-内酰胺的选择性抗癌活性。

Selective anticancer activity of β-lactams derived from polyaromatic compound.

机构信息

Department of Chemistry, The University of Texas Pan American, Edinburg, TX 78539, USA.

出版信息

Mol Med Rep. 2010 Mar-Apr;3(2):315-6. doi: 10.3892/mmr_00000257.

Abstract

Currently available anticancer drugs are cytotoxic to normal as well as to neoplastic cells, therefore the synthesis of β-lactams as new and novel anticancer agents is extremely significant. We previously developed synthetic methods for the preparation of β-lactams and anticancer agents resulting from polyaromatic amines. There have also been reports on the synthesis and biological evaluation of novel racemic β-lactams as anticancer agents. In cell cycle analysis, these compounds demonstrated a G2 blockage against sensitive tumor cell lines. In the present study, useful and selective biological activities of chrysene β-lactams are described.

摘要

目前可用的抗癌药物对正常细胞和肿瘤细胞都具有细胞毒性，因此合成β-内酰胺类抗生素作为新型抗癌药物具有非常重要的意义。我们之前开发了用于制备β-内酰胺类抗生素和多环芳烃衍生的抗癌药物的合成方法。也有报道称合成了新型外消旋β-内酰胺类抗生素作为抗癌药物，并对其进行了生物评价。在细胞周期分析中，这些化合物对敏感的肿瘤细胞系表现出 G2 阻断作用。在本研究中，描述了 chrysene β-内酰胺类抗生素的有用和选择性的生物活性。