两种新型杂环稠合（-）-鼠李糖酸类似物的设计、合成及抗增殖活性
Design, synthesis and antiproliferative activity of two new heteroannelated (-)-muricatacin mimics.
作者信息
Popsavin Velimir, Srećo Bojana, Benedeković Goran, Popsavin Mirjana, Francuz Jovana, Kojić Vesna, Bogdanović Gordana
机构信息
Department of Chemistry, Faculty of Sciences, University of Novi Sad, Trg D. Obradovića 3, 21000 Novi Sad, Serbia.
出版信息
Bioorg Med Chem Lett. 2008 Oct 1;18(19):5182-5. doi: 10.1016/j.bmcl.2008.08.097. Epub 2008 Aug 29.
Two new (-)-muricatacin mimics bearing a furano-furanone ring and an oxygen isostere in the side chain have been designed and synthesized and their in vitro antiproliferative activity was evaluated against several human tumour cell lines. Both analogues showed an increased activity against HL-60 cells with 17- and 185-fold higher potency than (-)-muricatacin. A straightforward synthesis of (-)-muricatacin is also disclosed.
设计并合成了两种新的（-）-muricatacin类似物，其侧链带有呋喃-呋喃酮环和氧类似物，并评估了它们对几种人类肿瘤细胞系的体外抗增殖活性。两种类似物对HL-60细胞均显示出增强的活性，其效力分别比（-）-muricatacin高17倍和185倍。还公开了（-）-muricatacin的一种直接合成方法。
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