Design, Synthesis and Biological Evaluation of Thiohydantoin Derivatives as Novel Anti-prostate Cancer Agents.

Abstract:

:A series of novel thiohydantoin derivatives were synthesized and evaluated for the abilities of inhibiting cell proliferation and prostate specific antigen (PSA) expression in prostate cancer cells. These derivatives selectively inhibited proliferation of AR positive LNCaP cells and PSA expression except compounds 5i and 5j. Compound 5t was approximately 15-fold more potent than MDV3100 to inhibit LNCaP cell proliferation. Compounds 5i and 5j inhibited cell growth of both AR positive LNCaP cells and AR negative PC-3 cells with potential to be developed as novel agents to treat antiandrogen resistant prostate cancer.

authors

Liu J,Liu B,Jing Y,Zhao G

doi

10.2174/1871520615666150803124622

subject

Has Abstract

pub_date

2016-01-01 00:00:00

pages

740-6

issue

6

eissn

1871-5206

issn

1875-5992

pii

ACAMC-EPUB-69275

journal_volume

16

pub_type

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