Antihormonal potential of selected D-homo and D-seco estratriene derivatives
| Autor: | Suzana Jovanović-Šanta, Mihály Szécsi, Olivera R. Klisurić, Radmila Kovacevic, Edward T. Petri, Julijana Petrovic |
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| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
Models
Molecular Stereochemistry medicine.drug_class Clinical Biochemistry Molecular Conformation Estrogen receptor Crystallography X-Ray 010402 general chemistry 01 natural sciences Biochemistry Structure-Activity Relationship 03 medical and health sciences Aromatase Hormone Antagonists 0302 clinical medicine Endocrinology In vivo medicine Animals Secosteroids 03.02. Klinikai orvostan Enzyme Inhibitors Estrenes Rats Wistar Molecular Biology Pharmacology chemistry.chemical_classification Dose-Response Relationship Drug biology Organic Chemistry Steroid 17-alpha-Hydroxylase Estrogens Stereoisomerism Lyase medicine.disease In vitro Rats 0104 chemical sciences 3. Good health Osteopenia Enzyme chemistry Estrogen 030220 oncology & carcinogenesis biology.protein Homosteroids Female |
| Popis: | 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 α (ERα), 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. |
| Databáze: | OpenAIRE |
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