Structure–activity relationships for withanolides as inducers of the cellular heat-shock response

EMK Wijeratne, YM Xu, R Scherz-Shouval…

文献索引：Wijeratne, E. M. Kithsiri; Xu, Ya-Ming; Scherz-Shouval, Ruth; Marron, Marilyn T.; Rocha, Danilo D.; Liu, Manping X.; Costa-Lotufo, Leticia V.; Santagata, Sandro; Lindquist, Susan; Whitesell, Luke; Gunatilaka, A. A. Leslie Journal of Medicinal Chemistry, 2014 , vol. 57, # 7 p. 2851 - 2863

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被引用次数: 23

摘要

To understand the relationship between the structure and the remarkably diverse bioactivities reported for withanolides, we obtained withaferin A (WA; 1) and 36 analogues (2–37) and compared their cytotoxicity to cytoprotective heat-shock-inducing activity (HSA). By analyzing structure–activity relationships for the series, we found that the ring A enone is essential for both bioactivities. Acetylation of 27-OH of 4-epi-WA (28) to 33 enhanced both ...