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Synthesis of novel galeterone derivatives and evaluation of their in vitro activity against prostate cancer cell lines
R. Jorda, E. Řezníčková, U. Kiełczewska, J. Maj, JW. Morzycki, L. Siergiejczyk, V. Bazgier, K. Berka, L. Rárová, A. Wojtkielewicz,
European journal of medicinal chemistry.
2019 ;
179 (-) :
483-492.
[pub] 20190618
Jazyk angličtina Země Francie
Typ dokumentu časopisecké články
Perzistentní odkaz
https://www.medvik.cz/link/bmc19044697
- MeSH
- androstadieny chemická syntéza chemie farmakologie MeSH
- benzimidazoly chemická syntéza chemie farmakologie MeSH
- buněčné linie MeSH
- buňky PC-3 MeSH
- lidé MeSH
- molekulární struktura MeSH
- nádory prostaty farmakoterapie metabolismus patologie MeSH
- proliferace buněk účinky léků MeSH
- protinádorové látky chemická syntéza chemie farmakologie MeSH
- screeningové testy protinádorových léčiv MeSH
- viabilita buněk účinky léků MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- mužské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
Prostate cancer is one of the main causes of male cancer-related deaths worldwide and the suppression of androgen receptor signalling is established as an effective strategy for the treatment. A series of galeterone analogues including several steroid-fused azacycles, as well as 17-(benzimidazol-1-ylimino), 16α-(benzimidazol-2-ylamino), and 16α-(benzothiazol-2-ylamino) steroid derivatives, were synthesized and tested against prostate cancer cell lines. Candidate compound 3f was shown to reduce AR-regulated transcription in a dose-dependent manner in nanomolar ranges and suppress expression of AR-regulated proteins Nkx3.1 and PSA in 22Rv1-ARE14 and VCaP cancer cell lines. Flexible docking study revealed similar position of 3f within AR binding site in comparison of galeterone even with stronger binding energy.
Citace poskytuje Crossref.org
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