TY  - JOUR
AU  - Jovanovic-Santa, SS
AU  - Petri, ET
AU  - Klisuric, OR
AU  - Szécsi, Mihály
AU  - Kovacevic, R
AU  - Petrovic, JA
TI  - Antihormonal potential of selected D-homo and D-seco estratriene derivatives
JF  - STEROIDS
J2  - STEROIDS
VL  - 97
PY  - 2015
SP  - 45
EP  - 53
PG  - 9
SN  - 0039-128X
DO  - 10.1016/j.steroids.2014.08.026
UR  - https://m2.mtmt.hu/api/publication/2829777
ID  - 2829777
N1  - Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Science, University of Novi Sad, Trg Dositeja Obradovića 3, Novi Sad, 21000, Serbia            
            Department of Biology and Ecology, Faculty of Science, University of Novi Sad, Trg Dositeja Obradovića 2, Novi Sad, 21000, Serbia            
            Department of Physics, Faculty of Science, University of Novi Sad, Trg Dositeja Obradovića 4, Novi Sad, 21000, Serbia            
            First Department of Medicine, University of Szeged, Korányi fasor 8-10, Szeged, H-6720, Hungary            
            Cited By :11            
            Export Date: 3 May 2022            
            CODEN: STEDA            
            Correspondence Address: Jovanović-Šanta, S.S.; Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Science, University of Novi Sad, Trg Dositeja Obradovića 3, Serbia            
            Chemicals/CAS: androstenedione, 26264-53-9, 63-05-8; aromatase, 9039-48-9; estradiol benzoate, 50-50-0; olive oil, 8001-25-0; steroid 17alpha monooxygenase, 189355-97-3, 9029-67-8, 9044-50-2, 331947-43-4, 9068-00-2; tamoxifen, 10540-29-1; Aromatase; Enzyme Inhibitors; Estrenes; Estrogens; Homosteroids; Hormone Antagonists; Secosteroids; Steroid 17-alpha-Hydroxylase            
            Manufacturers: Sigma, United States
AB  - Since many estrogen derivatives exhibit anti-hormone or enzyme inhibition potential, a large number of steroidal derivatives have been synthesised from appropriate precursors, in order to obtain potential therapeutics for the treatment of hormone-dependent cancers. In molecular docking studies, based on X-ray crystallographic analysis, selected D-homo and D-seco estratriene derivatives were predicted to bind strongly to estrogen receptor alpha (ERalpha), aromatase and 17,20 lyase, suggesting they could be good starting compounds for antihormonal studies. Test results in vivo suggest that these compounds do not possess estrogenic activity, while some of them showed weak anti-estrogenic properties. In vitro anti-aromatase and anti-lyase assays showed partial inhibition of these two enzymes, while some compounds activated aromatase. Aromatase activators are capable of promoting estrogen synthesis for treatment of pathological conditions caused by estrogen depletion, e.g. osteopenia or osteoporosis.
LA  - English
DB  - MTMT
ER  -