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Concise synthesis of polymethoxyflavone sudachitin and its derivatives, and biological evaluations
Tetrahedron Letters ( IF 1.8 ) Pub Date : 2018-03-24 , DOI: 10.1016/j.tetlet.2018.03.064
Hiroto Sagara , Masaki Kanakogi , Yuki Tara , Hitoshi Ouchi , Junko Kimura , Yukiko Kaneko , Makoto Inai , Tomohiro Asakawa , Tomohisa Ishikawa , Toshiyuki Kan

We accomplished a divergent synthesis of sudachitin (2), a polymethoxyflavone isolated from citrus fruits, and six derivatives from acetophenone 9, which was an intermediate in our previous synthesis of nobiletin (1). Compound 2 enhanced glucose-induced insulin secretion in INS-1D cells, but was less potent than 1. Compared with 1, compound 2 and two derivatives were more potent inhibitors of cAMP-specific phosphodiesterase.



中文翻译:

聚甲氧基黄酮Sudachitin及其衍生物的简捷合成及生物学评价

我们完成了sudachitin(2)(一种从柑橘类水果中分离出来的聚甲氧基黄酮)和六种苯乙酮9衍生物的衍生物的多样化合成,这是我们之前合成nobiletin(1)的中间体。化合物2增强了INS-1D细胞中葡萄糖诱导的胰岛素分泌,但作用强度低于1。与1相比,化合物2和两个衍生物是cAMP特异性磷酸二酯酶的更有效抑制剂。

更新日期:2018-03-24
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