Murphy Annabel C, Devenish Sean R A, Muscroft-Taylor Andrew C, Blunt John W, Munro Murray H G
Department of Chemistry, University of Canterbury, Christchurch, New Zealand.
Org Biomol Chem. 2008 Oct 21;6(20):3854-62. doi: 10.1039/b812263f. Epub 2008 Sep 3.
An exploration of the chemistry of the spiro-mamakone system, exemplified by the cytotoxic, fungal metabolite spiro-mamakone A, is presented. The first reported synthesis of the spiro-mamakone carbon skeleton was achieved, as well as the synthesis of a variety of closely related analogues of the natural product. Biological testing of the synthetic analogues generated a structure-activity profile for the natural product, establishing the importance of the enedione moiety to biological activity.
本文介绍了以具有细胞毒性的真菌代谢产物螺-马马酮A为例的螺-马马酮体系的化学研究。首次实现了螺-马马酮碳骨架的合成，以及该天然产物多种密切相关类似物的合成。对合成类似物的生物学测试得出了该天然产物的构效关系，确立了烯二酮部分对生物活性的重要性。
