当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis of novel galeterone derivatives and evaluation of their in vitro activity against prostate cancer cell lines.

Synthesis of novel galeterone derivatives and evaluation of their in vitro activity against prostate cancer cell lines.

Abstract：

: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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Jorda R,Řezníčková E,Kiełczewska U,Maj J,Morzycki JW,Siergiejczyk L,Bazgier V,Berka K,Rárová L,Wojtkielewicz A

doi

10.1016/j.ejmech.2019.06.040

subject

Has Abstract

pub_date

2019-10-01 00:00:00

pages

483-492

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(19)30566-5

journal_volume

179

pub_type

杂志文章

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