%A  MernyĂĄk ErzsĂŠbet
%A  SzabĂł Johanna
%A  Bacsa IldikĂł
%A  Huber Judit
%A  Schneider Gyula
%A  Minorics RenĂĄta
%A  BĂłzsity NoĂŠmi
%A  ZupkĂł IstvĂĄn
%A  Varga MĂłnika
%A  BikĂĄdi Zsolt
%A  Hazai Eszter
%A  WĂślfling JĂĄnos
%T Syntheses and Antiproliferative Effects of D-homo- and D-secoestrones
%L publicatio8318
%P 128-136
%V 87
%J STEROIDS
%N 0
%D 2014
%X 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.
%I szte
%O FELTÖLTŐ: Bózsity Noémi - bozsity.noemi@pharm.u-szeged.hu
%R 2602154