94838-67-2Relevant academic research and scientific papers
Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors
Xiang, Qiuping,Luo, Guolong,Zhang, Cheng,Hu, Qingqing,Wang, Chao,Wu, Tianbang,Xu, Hongrui,Hu, Jiankang,Zhuang, Xiaoxi,Zhang, Maofeng,Wu, Shuang,Xu, Jinxin,Zhang, Yan,Liu, Jinsong,Xu, Yong
, (2022/04/07)
TRIM24 (tripartite motif-containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are epigenetics “readers” and potential therapeutic targets for cancer and other diseases. Here we describe the structure-guided design of 1-(indolin-1-yl)ethan-1-ones as novel TRIM24/BRPF1 bromodomain inhibitors. The representative compound 20l (Y08624) is a new TRIM24/BRPF1 dual inhibitor, with IC50 values of 0.98 and 1.16 μM, respectively. Cellular activity of 20l was validated by viability assay in prostate cancer (PC) cell lines. In PC xenograft models, 20l suppressed tumor growth (50 mg/kg/day, TGI = 53%) without exhibiting noticeable toxicity. Compound 20l represents a versatile starting point for the development of more potent TRIM24/BRPF1 inhibitors.
Ruthenium-catalyzed meta/ortho-selective C-H alkylation of azoarenes using alkyl bromides
Li, Gang,Ma, Xingxing,Jia, Chunqi,Han, Qingqing,Wang, Ya,Wang, Junjie,Yu, Liuyang,Yang, Suling
, p. 1261 - 1264 (2017/02/05)
meta/ortho-Selective CAr-H (di)alkylation reactions of azoarenes have been achieved via [Ru(p-cymene)Cl2]2 catalyzed ortho-metalation using various types of alkyl bromides. Particularly, dual meta-alkylation of azoarene and reduction offer an attractive strategy for the synthesis of meta-alkylanilines, which are difficult to access via traditional aniline functionalization methods.
4-PHENYL-PYRIMIDINE-2-CARBONITRILE DERIVATIVES
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Page/Page column 59, (2008/06/13)
The invention relates to 4-phenyl-pyrimidine-2-carbonitrile derivatives having the general formula (I) or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives as well as to the use thereof in the preparation of a medicament suitable for the treatment of osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.
