1295570-35-2Relevant academic research and scientific papers
DIARYLTHIOHYDANTOIN COMPOUND AS ANDROGEN RECEPTOR ANTAGONIST
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Paragraph 0271; 0274-0275, (2020/07/07)
The present application belongs to the field of medicine. In particular, the present application relates to a diarylthiohydantoin compound as an androgen receptor antagonist or a pharmaceutically acceptable salt thereof, a preparation method of the same, a pharmaceutical composition comprising the compound, and a use thereof in treating a cell proliferative disease mediated by androgen. The compound of the present application has good antagonistic effect on androgen receptor and exhibits excellent antitumor effect.
Synthesis and biological evaluation of 4-quinazolinones as Rho kinase inhibitors
Fang, Xingang,Chen, Yen Ting,Sessions, E. Hampton,Chowdhury, Sarwat,Vojkovsky, Tomas,Yin, Yan,Pocas, Jennifer R.,Grant, Wayne,Schr?ter, Thomas,Lin, Li,Ruiz, Claudia,Cameron, Michael D.,Lograsso, Philip,Bannister, Thomas D.,Feng, Yangbo
, p. 1844 - 1848 (2011/05/05)
Rho kinase (ROCK) is an attractive therapeutic target for various diseases including glaucoma, hypertension, and spinal cord injury. Herein, we report the development of a series of ROCK-II inhibitors based on 4-quinazolinone and quinazoline scaffolds. SAR studies at three positions of the quinazoline core led to the identification of analogs with high potency against ROCK-II and good selectivity over protein kinase A (PKA).
