کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2027809 | 1542720 | 2014 | 9 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Syntheses and antiproliferative effects of d-homo- and d-secoestrones Syntheses and antiproliferative effects of d-homo- and d-secoestrones](/preview/png/2027809.png)
• Synthesis of d-homoestrones via the intramolecular cyclization of d-secoestrones.
• Significant in vitro antiproliferative effect of d-homo and d-secoestrones.
• Enhancement of the maximum rate of in vitro formation of microtubules.
Substituted and/or heterocyclic d-homoestrone derivatives were synthetized via the intramolecular cyclization of a δ-alkenyl-d-secoaldehyde, -d-secoalcohol or -d-secocarboxylic acid of estrone 3-benzyl ether. The d-secoalcohol was modified at three sites in the molecule. The in vitro antiproliferative activities of the new d-homo- and d-secoestrone derivatives were determined on HeLa, MCF-7, A431 and A2780 cells through use of MTT assay. d-Homoalcohols 3 and 5 displayed cell line-selective cytostatic effects against ovarian and cervical cell lines, respectively. Two d-secoestrones (6 and 12c) proved to be effective, with IC50 values comparable with those of the reference agent cisplatin. A selected compound (6) was tested by tubulin polymerization assay and its cancer specificity was additionally determined by using noncancerous human fibroblast cells.
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Journal: Steroids - Volume 87, September 2014, Pages 128–136