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首页> 外文期刊>RSC Advances >Synthesis and biological evaluation of 4 beta-benzoxazolepodophyllotoxin hybrids as DNA topoisomerase-II targeting anticancer agents
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Synthesis and biological evaluation of 4 beta-benzoxazolepodophyllotoxin hybrids as DNA topoisomerase-II targeting anticancer agents

机译：4β-苯并恶唑哌肺素杂种的合成及生物学评价为DNA Topoisomerase-II靶向抗癌剂

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摘要

A series of new 4 beta-benzoxazolepodophyllotoxin compounds (9a-j) were prepared and screened for cytotoxicity against four human tumour cell lines (HeLa, DU-145, A-159 and MCF-7). Among these compounds, 9a, 9c, 9f and 9i have shown more potent anticancer activity than etoposide with considerable IC50 values. Apoptosis evaluation studies were performed using the Hoechst-33258 staining method and it was found specially that the best active compound 9i shows clear nuclear damage compared to etoposide. Molecular docking studies were also carried out to recognize the interactions against DNA topoisomerase-II and it was found that the energy calculations were in good agreement with the observed IC50 value.
机译：制备了一系列新的4β-苯并恶唑己唑曲霉毒素（9A-J）并筛选细胞毒性，用于四种人肿瘤细胞系（Hela，Du-145，A-159和MCF-7）。 在这些化合物中，9A，9C，9F和9I具有比具有相当大的IC50值的依托肽更有效的抗癌活性。 使用Hoechst-33258染色方法进行细胞凋亡评估研究，特别是与依托泊苷相比，最好的活性化合物9i显示出明显的核损伤。 还进行了分子对接研究以识别对DNA拓扑异构酶-II的相互作用，并发现能量计算与观察到的IC50值吻合良好。

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