Synthesis of sominone and its derivatives based on an RCM strategy: discovery of a novel anti-Alzheimer's disease medicine candidate "denosomin".
Synthesis of sominone and its derivatives based on an RCM strategy: discovery of a novel anti-Alzheimer's disease medicine candidate "denosomin".
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DOI：
10.1021/ol901553w
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发表时间：
2009-08
期刊：
影响因子：
5.2
通讯作者：
Y. Matsuya;Y. Yamakawa;C. Tohda;K. Teshigawara;M. Yamada;H. Nemoto*
中科院分区：
文献类型：
--
作者：
Y. Matsuya;Y. Yamakawa;C. Tohda;K. Teshigawara;M. Yamada;H. Nemoto*
基于用于构建δ-内酯侧链的RCM策略，从脱氢表雄酮开始实现索米酮的合成。该合成方案被应用于几个类似的衍生物，包括1-脱氧-24-norsominone（denosomin）的合成，这是显示出显着的新的抗痴呆化疗的生物活性，超过了原来的天然化合物sominone。
Synthesis of sominone was achieved starting from dehydroepiandrosterone on the basis of an RCM strategy for the construction of a delta-lactone side chain. This synthetic protocol was applied for the synthesis of several analogous derivatives including 1-deoxy-24-norsominone (denosomin), which was revealed to exhibit notable bioactivities for new antidementia chemotherapy, exceeding the original natural compound sominone.