（R）-角鲨胺：全合成及其对癌细胞系的细胞毒性活性
(R)-Goniothalamin: total syntheses and cytotoxic activity against cancer cell lines.
作者信息
de Fátima Angelo, Kohn Luciana Konecny, Antônio Márcia Aparecida, de Carvalho João Ernesto, Pilli Ronaldo Aloise
机构信息
Instituto de Química, Unicamp, CP 6154, 13084-971, Campinas, São Paulo, Brazil.
出版信息
Bioorg Med Chem. 2005 Apr 15;13(8):2927-33. doi: 10.1016/j.bmc.2005.02.007.
The total syntheses of (R)-goniothalamin (1), a styryl lactone isolated from several Goniothalamus species, via catalytic asymmetric allylation of alpha-benzyloxyacetaldehyde (2), followed by ring-closing metathesis and Wittig olefination and via catalytic asymmetric allylation of trans-cinnamaldehyde (12), followed by ring-closing metathesis are reported. The antiproliferative activities of (R)-1 and its Z-isomer 10 as well as of the synthetic dihydropyranone intermediates 7 and 8 against eight different cancer cell lines are also described.
从几种哥纳香属植物中分离得到的苯乙烯基内酯（R）-戈尼他胺（1）的全合成方法被报道，该方法通过α-苄氧基乙醛（2）的催化不对称烯丙基化反应，随后进行闭环复分解反应和维蒂希烯烃化反应，以及通过反式肉桂醛（12）的催化不对称烯丙基化反应，随后进行闭环复分解反应。还描述了（R）-1及其Z-异构体10以及合成二氢吡喃酮中间体7和8对八种不同癌细胞系的抗增殖活性。
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