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Expeditious Synthesis of Hippuristanol and Congeners with Potent Antiproliferative Activities

机译:快速合成具有强大抗增殖活性的庚嘌呤醇和同类物

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摘要

Hippuristanol (1) and its congeners comprise a family ofstructurally unique polyoxygenated steroids isolated fromthe Gorgonian Isis hippuris with potent antiproliferative ac-tivity against different cancer cell lines in vitro.~[1]The molec-ular basis of their antiproliferative activity, however, re-mained a mystery until recently. Hippuristanol was reportedto target the eukaryotic translation initiation factor(eIF)4A,~[2a,b]an ATP-dependent RNA helicase that plays apivotal role in translation in eukaryotic cells. The discoveryof hippuristanol, along with another marine sponge-derivednatural product pateamine A, as inhibitors of eukaryotictranslation, not only offered new molecular probes to studyeukaryotic translation initiation mediated by eIF4A, butalso had important implications in targeting the translationprocess for the development of novel anticancer and antivi-ral drugs.
机译:Hippuristanol(1)及其同类物包含一类结构独特的多加氧类固醇,它们是从Gorgonian Isis hippuris中分离出来的,在体外对不同癌细胞系具有强抗增殖活性。[1]其抗增殖活性的分子基础是-直到最近一直是一个谜。据报道,高嘌呤醇靶向真核翻译起始因子(eIF)4A,〜[2a,b]一种ATP依赖性RNA解旋酶,在真核细胞的翻译中起重要作用。马斯普林醇以及另一种海洋海绵衍生的天然产物帕他明A作为真核翻译抑制剂的发现,不仅为研究由eIF4A介导的真核翻译起始提供了新的分子探针,而且对于靶向翻译过程以开发新型抗癌和抗病毒药物也具有重要意义。 -ral药物。

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