1190380-38-1Relevant articles and documents
Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer
Wang, Ao,Wang, Yawan,Meng, Xin,Yang, Yushe
, (2021)
Prostate cancer (PC) is the most common malignancy in men worldwide. Here, two series of novel thiohydantoin derivatives of enzalutamide as potent androgen receptor (AR) antagonists were designed and synthesized. Among them, compound 31c was identified as an AR antagonist which is 2.3–fold more potent than enzalutamide. Molecular docking studies were performed to explain the improved potency of 31c at AR. In cell proliferation assays, 31c exhibited similar anti-proliferative activities with enzalutamide against hormone sensitive LNCaP cells and AR-overexpressing LNCaP/AR cells. These data indicate that 31c can be a good lead compound for further structure optimization for the treatment of prostate cancer.
Diarylurea PI3Kalpha/mTOR double-target inhibitor and pharmaceutical composition, and application of inhibitor and pharmaceutical composition
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Paragraph 0168-0172; 0183-0186, (2021/07/01)
The invention discloses a diarylurea PI3Kalpha/mTOR double-target inhibitor as well as a pharmaceutical composition, and application of the diarylurea PI3K alpha/mTOR double-target inhibitor and the pharmaceutical composition. The diarylurea PI3Kalpha/mTOR double-target inhibitor comprises a substituted triazine compound with a general formula (I) described in the specification, and a stereoisomer, a hydrate or a pharmaceutically acceptable salt thereof. The diarylurea PI3Kalpha/mTOR double-target inhibitor provided by the invention and the pharmaceutical composition containing the diarylurea PI3K alpha/mTOR double-target inhibitor can be used for inhibiting PI3Kalpha/mTOR double kinase and proliferative diseases caused by the PI3Kalpha/mTOR double kinase, and an inhibitor with better effectiveness and selectivity can be provided for treatment of the PI3Kalpha/mTOR double-kinase-induced proliferative diseases.
HETEROARYL COMPOUNDS AND USES THEREOF
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, (2016/06/28)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are effective as inhibitors of one or more protein kinases. Such compounds have general formula I or a pharmaceutically acceptable salt thereof, wherein Ring A, Ring B, W, Ry, R3 and R4 are as defined herein.