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

作者:Gong Jun; Sun Peng; Jiang Nan; Riccio Raffaele; Lauro Gianluigi; Bifulco Giuseppe; Li Tie Jun; Gerwick William H; Zhang Wen*
来源:Organic Letters, 2014, 16(8): 2224-2227.
DOI:10.1021/ol5007345

摘要

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%26apos;s 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.