Structure activity relationship studies on cytotoxicity and the effects on steroid receptors of AB-functionalized cholestanes
Jazyk angličtina Země Velká Británie, Anglie Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
26976651
DOI
10.1016/j.jsbmb.2016.03.017
PII: S0960-0760(16)30063-2
Knihovny.cz E-zdroje
- Klíčová slova
- Antiproliferative activity, Apoptosis, Cell cycle, Cholestane derivatives, Steroid receptor, Structure-activity relationship,
- MeSH
- antitumorózní látky chemie farmakologie MeSH
- apoptóza MeSH
- buněčný cyklus účinky léků MeSH
- cholestany chemie farmakologie MeSH
- inhibiční koncentrace 50 MeSH
- léky antitumorózní - screeningové testy MeSH
- lidé MeSH
- nádorové buněčné linie MeSH
- steroidní receptory metabolismus MeSH
- viabilita buněk MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- antitumorózní látky MeSH
- cholestany MeSH
- steroidní receptory MeSH
Structure-activity relationship analysis and profiling of a library of AB-functionalized cholestane derivatives closely related to brassinosteroids (BRs) were performed to examine their antiproliferative activities and activities on steroid hormone receptors. Some of the compounds were found to have strong cytotoxic activity in several human normal and cancer cell lines. The presence of a 3-hydroxy or 3-oxo group and 2,3-vicinal diol or 3,4-vicinal diol moiety were found to be necessary for optimum biological activity, as well as a six-membered B ring. According to the profiling of all steroid receptors in both agonist and antagonist mode, the majority of the cholestanes were weakly active or inactive compared to the natural ligands. Estrogenic activity was detected for two compounds, two compounds possessed antagonistic properties on estrogen receptors and seven compounds showed agonistic activity. Two active cholestane derivatives were shown to strongly influence cell viability, proliferation, cell cycle distribution, apoptosis and molecular pathways responsible for these processes in hormone-sensitive/insensitive (MCF7/MDA-MB-468) breast cancer cell lines.
Citace poskytuje Crossref.org
Cytokinin Plant Hormones Have Neuroprotective Activity in In Vitro Models of Parkinson's Disease
Synthesis and Biological Activity of Brassinosteroid Analogues with a Nitrogen-Containing Side Chain
Bioactive Steroids from the Red Sea Soft Coral Sinularia polydactyla
Synthesis of New Cisplatin Derivatives from Bile Acids
