کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1396402 | 1501187 | 2010 | 8 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Design, synthesis and antiproliferative activity of styryl lactones related to (+)-goniofufurone Design, synthesis and antiproliferative activity of styryl lactones related to (+)-goniofufurone](/preview/png/1396402.png)
This paper describes a straightforward divergent synthesis of (+)-goniofufurone mimics (4, 5 and 6) starting from d-xylose. In a preliminary bioassay, analogues 4 and 5 exhibited a submicromolar antiproliferative activity towards HL-60 cells, while the corresponding parent compound 1 was completely inactive against this cell line. At the same time, these molecules showed approximately 10-fold stronger cytotoxicity in the same cell line when compared to the standard anticancer drug doxorubicin (DOX). Analogue 6 displayed 18- and 3-fold higher potency in Raji cell line when compared to control compounds 1 and DOX, respectively. A new divergent route for the preparation of (+)-goniofufurone (1) and (+)-crassalactone C (3) from d-xylose is also disclosed.
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Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 7, July 2010, Pages 2876–2883