苯并[g][1]苯并吡喃[4,3-b]吲哚-6(13H)-酮（BBPIs）的简洁合成及体外抗癌活性，基于海洋生物碱拉米林的拓扑异构酶 I 抑制剂。
Concise synthesis and in vitro anticancer activity of benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-ones (BBPIs), topoisomerase I inhibitors based on the marine alkaloid lamellarin.
机构信息
Graduate School of Fisheries and Environmental Sciences, Nagasaki University, Nagasaki, Japan.
Environmental Protection Center, Nagasaki University, Nagasaki, Japan.
出版信息
Biosci Biotechnol Biochem. 2021 Jan 7;85(1):181-191. doi: 10.1093/bbb/zbaa028.
Benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-ones (BBPIs) are potent anticancer compounds having unique BBPIs ring system designed on the basis of the marine natural product lamellarin D. In this study, we describe an alternative synthesis of a 2-demethoxy series of BBPIs, employing van Leusen pyrrole synthesis and an intramolecular Heck reaction as the key reactions. Cytotoxicity of the derivatives against several cancer and normal cell lines is reported.
苯并[g][1]苯并吡喃[4,3-b]吲哚-6(13H)-酮（BBPIs）是具有独特 BBPIs 环系的强效抗癌化合物，该环系是基于海洋天然产物拉米林 D 设计的。在这项研究中，我们描述了一种替代的 2-去甲氧基系列 BBPIs 的合成方法，采用范吕森吡咯合成和分子内 Heck 反应作为关键反应。报道了衍生物对几种癌细胞和正常细胞系的细胞毒性。
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