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...

Teljes leírás

Elmentve itt :
Bibliográfiai részletek
Szerzők: Mernyák Erzsébet
Szabó Johanna
Bacsa Ildikó
Huber Judit
Schneider Gyula
Minorics Renáta
Bózsity Noémi
Zupkó István
Varga Mónika
Bikádi Zsolt
Hazai Eszter
Wölfling János
Dokumentumtípus: Cikk
Megjelent: 2014
Sorozat:STEROIDS 87 No. 0
doi:10.1016/j.steroids.2014.05.015

mtmt:2602154
Online Access:http://publicatio.bibl.u-szeged.hu/8318
LEADER 01954nab a2200337 i 4500
001 publ8318
005 20190517123326.0
008 170329s2014 hu o 0|| angol d
022 |a 0039-128X 
024 7 |a 10.1016/j.steroids.2014.05.015  |2 doi 
024 7 |a 2602154  |2 mtmt 
040 |a SZTE Publicatio Repozitórium  |b hun 
041 |a angol 
100 1 |a Mernyák Erzsébet 
245 1 0 |a Syntheses and Antiproliferative Effects of D-homo- and D-secoestrones  |h [elektronikus dokumentum] /  |c  Mernyák Erzsébet 
260 |c 2014 
300 |a 128-136 
490 0 |a STEROIDS  |v 87 No. 0 
520 3 |a 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. 
700 0 1 |a Szabó Johanna  |e aut 
700 0 1 |a Bacsa Ildikó  |e aut 
700 0 1 |a Huber Judit  |e aut 
700 0 1 |a Schneider Gyula  |e aut 
700 0 1 |a Minorics Renáta  |e aut 
700 0 1 |a Bózsity Noémi  |e aut 
700 0 1 |a Zupkó István  |e aut 
700 0 1 |a Varga Mónika  |e aut 
700 0 1 |a Bikádi Zsolt  |e aut 
700 0 1 |a Hazai Eszter  |e aut 
700 0 1 |a Wölfling János  |e aut 
856 4 0 |u http://publicatio.bibl.u-szeged.hu/8318/1/Steroids_dhomo_seco_u.pdf  |z Dokumentum-elérés