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Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2

โœ Scribed by Nasveschuk, Christopher G.; Gagnon, Alexandre; Garapaty-Rao, Shivani; Balasubramanian, Srividya; Campbell, Robert; Lee, Christina; Zhao, Feng; Bergeron, Louise; Cummings, Richard; Trojer, Patrick; Audia, James E.; Albrecht, Brian K.; Harmange, Jean-Christophe P.


Book ID
124082837
Publisher
American Chemical Society
Year
2014
Tongue
English
Weight
930 KB
Volume
5
Category
Article
ISSN
1948-5875

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โœ Peter J. Tummino; J.V.N. Vara Prasad; Donna Ferguson; Carolyn Nouhan; Neil Graha ๐Ÿ“‚ Article ๐Ÿ“… 1996 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 779 KB

Several small, achiral nonpeptide inhibitors of HIV-1 protease with low micromolar activity were identified by mass screening of the Parke-Davis compound library. Two of the compounds, structurally similar, were both found to be competitive and reversible inhibitors [compound 1, 4-hydroxy-3-(3-pheno