New Steroids with a Rearranged Skeleton as (h)P300 Inhibitors from the Sponge Theonella swinhoei

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• 作者：Jun Gong ; Peng Sun ; Nan Jiang ; Raffaele Riccio ; Gianluigi Lauro ; Giuseppe Bifulco ; Tie-Jun Li ; William H. Gerwick ; Wen Zhang
• 刊名：Organic Letters
• 出版年：2014
• 出版时间：April 18, 2014
• 年：2014
• 卷：16
• 期：8
• 页码：2224-2227
• 全文大小：306K
• 年卷期：v.16,no.8(April 18, 2014)
• ISSN：1523-7052

文摘

Swinhoeisterols A (1) and B (2), two novel sterols with an unprecedented 6/6/5/7 ring system, were isolated from the sponge Theonella swinhoei. The structures and absolute configurations were elucidated by spectroscopic analysis, X-ray single-crystal diffraction, modified Mosher鈥檚 method, and TDDFT/ECD calculations. The cytotoxicity of these compounds toward A549 and MG-63 cells encourages studies on their potential target using an inverse virtual screening approach. The predicted inhibitor of h(p300) was corroborated by an in vitro biological test.