1355338-16-7Relevant articles and documents
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton
Nishiyama, Yuko,Mori, Shuichi,Makishima, Makoto,Fujii, Shinya,Kagechika, Hiroyuki,Hashimoto, Yuichi,Ishikawa, Minoru
, p. 641 - 645 (2018)
The progesterone receptor (PR) plays an important role in various physiological systems, including female reproduction and the central nervous system, and PR antagonists are thought to be effective not only as contraceptive agents and abortifacients but also in the treatment of various diseases, including hormone-dependent cancers and endometriosis. Here, we identified phenanthridin-6(5H)-one derivatives as a new class of PR antagonists and investigated their structure-activity relationships. Among the synthesized compounds, 37, 40, and 46 exhibited very potent PR antagonistic activity with high selectivity for PR over other nuclear receptors. These compounds are structurally distinct from other nonsteroidal PR antagonists, including cyanoaryl derivatives, and should be useful for further studies of the clinical utility of PR antagonists.
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγInverse Agonist for Treatment of Castration-Resistant Prostate Cancer
Zhang, Yan,Wu, Xishan,Xue, Xiaoqian,Li, Chenchang,Wang, Junjian,Wang, Rui,Zhang, Cheng,Wang, Chao,Shi, Yudan,Zou, Lingjiao,Li, Qiu,Huang, Zenghong,Hao, Xiaojuan,Loomes, Kerry,Wu, Donghai,Chen, Hong-Wu,Xu, Jinxin,Xu, Yong
, p. 4716 - 4730 (2019/05/08)
We report the design, optimization, and biological evaluation of nuclear receptor RORγinverse agonists as therapeutic agents for prostate cancer treatment. The most potent compound 27 (designated as XY101) exhibited cellular activity with an IC50/su
METHODS FOR TREATING CANCER WITH RORGAMMA INHIBITORS
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Paragraph 0188, (2017/09/02)
The present invention provides compositions, methods, and kits comprising one or more compounds of Formula I, such as XY018, alone or in combination with one or more anticancer drugs, such as an anti-androgen drug, that are useful for treating cancer, e.g., prostate cancer, such as castration-resistant prostate cancer (CRPC), and numerous other types of cancer including lung cancer, breast cancer, liver cancer, ovarian cancer, endometrial cancer, bladder cancer, colon cancer, gastric cancer, lymphoma, and glioma.