Syntheses and Antiproliferative Effects of D-homo- and D-secoestrones
Abstract 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 antipr...
Elmentve itt :
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| Dokumentumtípus: | Cikk |
| Megjelent: |
2014
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| Sorozat: | STEROIDS
87 No. 0 |
| doi: | 10.1016/j.steroids.2014.05.015 |
| mtmt: | 2602154 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/8318 |
| Tartalmi kivonat: | Abstract 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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| Terjedelem/Fizikai jellemzők: | 128-136 |
| ISSN: | 0039-128X |