Total Synthesis of Englerin A
Total Synthesis of Englerin A
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DOI：
10.1021/ja102927n
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发表时间：
2010-06-16
影响因子：
15
通讯作者：
Chen, David Y. -K.
中科院分区：
文献类型：
--
作者：
Nicolaou, K. C.;Kang, Qiang;Chen, David Y. -K.
Total synthesis of englerin A, a recently reported sesquiterpenoid exhibiting potent and selective growth inhibition against renal cancer cell lines, has been accomplished. The successful strategy featured a [5 + 2] cycloaddition reaction to cast the seven-membered oxabicyclic key intermediate in both racemic and optically active forms. Synthetic (+/-)-englerin A, (+/-)-englerin B, (+/-)-englerin B acetate, a hydroxy acetate, a tert-butyldimethylsilyl ether, and hydrogenated (+/-)-englerin A (31) were tested for their cytotoxicity against a selected panel of cancer cell lines, and the results are path-pointing to more focused structure-activity relationship studies.
