6140-11-0Relevant articles and documents
PROCESS AND INTERMEDIATES FOR THE PREPARATION OF BOC-LINAGLIPTIN
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Page/Page column 7; 8, (2020/03/02)
This invention relates to novel processes for the synthesis of Linagliptin, the pharmaceutically active ingredient, and the key intermediate thereof, BOC-Linagliptin. (I) The processes are performed via new intermediate compounds of Formula (5) and Formula (3).
Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization
Mao, Ruifeng,Shao, Jingwei,Zhu, Kongkai,Zhang, Yuanyuan,Ding, Hong,Zhang, Chenhua,Shi, Zhe,Jiang, Hualiang,Sun, Dequn,Duan, Wenhu,Luo, Cheng
, p. 6289 - 6304 (2017/08/02)
PRMT5 plays important roles in diverse cellular processes and is upregulated in several human malignancies. Besides, PRMT5 has been validated as an anticancer target in mantle cell lymphoma. In this study, we found a potent and selective PRMT5 inhibitor by performing structure-based virtual screening and hit optimization. The identified compound 17 (IC50 = 0.33 μM) exhibited a broad selectivity against a panel of other methyltransferases. The direct binding of 17 to PRMT5 was validated by surface plasmon resonance experiments, with a Kd of 0.987 μM. Kinetic experiments indicated that 17 was a SAM competitive inhibitor other than the substrate. In addition, 17 showed selective antiproliferative effects against MV4-11 cells, and further studies indicated that the mechanism of cellular antitumor activity was due to the inhibition of PRMT5 mediated SmD3 methylation. 17 may represent a promising lead compound to understand more about PRMT5 and potentially assist the development of treatments for leukemia indications.
A convenient method for the preparation of 3-phenoxy/thiophenoxy-2 (1H)-quinolinones
Riaz Hashim,Tirupathy Reddy
, p. 357 - 360 (2007/10/03)
A number of new 4-methyl-3-phenoxy/thiophenoxy-2 (1H) quinolinones have been synthesized in excellent yields through a simple and efficient procedure from N-(2-acetylphenyl)-phenoxy/thiophenoxy acetamides under basic conditions.