Synthesis of novel galeterone derivatives and evaluation of their in vitro activity against prostate cancer cell lines
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389030%3A_____%2F19%3A00509260" target="_blank" >RIV/61389030:_____/19:00509260 - isvavai.cz</a>
Alternative codes found
RIV/61989592:15310/19:73598517
Result on the web
<a href="http://dx.doi.org/10.1016/j.ejmech.2019.06.040" target="_blank" >http://dx.doi.org/10.1016/j.ejmech.2019.06.040</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.ejmech.2019.06.040" target="_blank" >10.1016/j.ejmech.2019.06.040</a>
Alternative languages
Result language
angličtina
Original language name
Synthesis of novel galeterone derivatives and evaluation of their in vitro activity against prostate cancer cell lines
Original language description
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.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10401 - Organic chemistry
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2019
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
European Journal of Medicinal Chemistry
ISSN
0223-5234
e-ISSN
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Volume of the periodical
179
Issue of the periodical within the volume
OCT 1
Country of publishing house
FR - FRANCE
Number of pages
10
Pages from-to
483-492
UT code for WoS article
000486133100033
EID of the result in the Scopus database
2-s2.0-85068166337