41013-95-0Relevant academic research and scientific papers
Discovery and optimization of selective inhibitors of protein arginine methyltransferase 5 by docking-based virtual screening
Ye, Yan,Zhang, Bidong,Mao, Ruifeng,Zhang, Chenhua,Wang, Yulan,Xing, Jing,Liu, Yu-Chih,Luo, Xiaomin,Ding, Hong,Yang, Yaxi,Zhou, Bing,Jiang, Hualiang,Chen, Kaixian,Luo, Cheng,Zheng, Mingyue
, p. 3648 - 3661 (2017)
Protein arginine methyltransferase 5 (PRMT5) is a type II PRMT enzyme critical for diverse cellular processes and different types of cancers. Many efforts have been made to discover novel scaffold PRMT5 inhibitors. Herein, we report the discovery of DC-P33 as a hit compound of PRMT5 inhibitor, identified by molecular docking based virtual screening and 3H-labeled radioactive methylation assays. Structure-activity relationship (SAR) analysis was performed on the analogs of DC-P33 and then structural modifications were done to improve its activity. Among the derivatives, the compound DC-C01 displayed an IC50 value of 2.8 μM, and good selectivity toward PRMT1, EZH2 and DNMT3A. Moreover, DC-C01 exhibited anti-proliferation activities against Z-138, Maver-1, and Jeko-1 cancer cells with EC50 values of 12 μM, 12 μM, and 10.5 μM, respectively. Taken together, these results contribute to the development of specific inhibitors against PRMT5 and cancer therapy.
SUBSTITUTED ANILINIC PIPERIDINES AS MCH SELECTIVE ANTAGONISTS
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Page column 166; 167, (2010/02/06)
This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therepeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.
Certain substituted 2-phenylnaphtho[1,2-b]furane and -[2,1-b]furane
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, (2008/06/13)
2-Phenylnaphtho[1,2-b]furan, 2-phenylnaphtho[2,1-b]-furan and derivatives thereof substituted in the phenyl ring by alkyl, halo or cyano are useful as antifertility agents, and are prepared by cyclization of a naphthyloxyacetophenone with a strong acid.
