Zobrazeno 1 - 3
of 3
pro vyhledávání: '"Oana Cociorva"'
Autor:
Kevin R. Shreder, Tyzoon K. Nomanbhoy, Ayako Nakamura, Anna Katrin Szardenings, Shigeki Seto, Jonathan S. Rosenblum, Brandon Leen, Oana Cociorva, Kai Nakamura, Bei Li, Marek Liyanage, John W. Kozarich, Qiang Li, Yasushi Kohno, Kazuhiro Yumoto, Kyoko Okada, Masahiro Nomura, Melissa C. Zhang, Arwin Aban
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5948-5951
The synthesis, GSK-3β inhibitory activity, and anti-microbial activity of bicyclic and tricyclic derivatives of the 5,7-diamino-6-fluoro-4-quinolone-3-carboxylic acid scaffold were studied. Kinase selectivity profiling indicated that members of this
Autor:
Kai Nakamura, Qiang Li, Tyzoon K. Nomanbhoy, Ann Yu-Jung Shih, Helge Weissig, Oana Cociorva, Lan Pham, John W. Kozarich, Yi Hu, Melissa C. Zhang, Marek Liyanage, Julia Cajica, Kevin R. Shreder, Arwin Aban, Bei Li
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(18)
As the result of a rhJNK1 HTS, the imidazo[1,2-a]quinoxaline 1 was identified as a 1.6 μM rhJNK1 inhibitor. Optimization of this compound lead to AX13587 (rhJNK1 IC50 = 160 nM) which was co-crystallized with JNK1 to identify key molecular interactio
Autor:
Tyzoon K. Nomanbhoy, Melissa C. Zhang, Kai Nakamura, Oana Cociorva, Kazuhiro Yumoto, Anna Katrin Szardenings, John W. Kozarich, Bei Li, Marek Liyanage, Yasushi Kohno, Kyoko Okada, Kevin R. Shreder, Masahiro Nomura, Qiang Li, Arwin Aban
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(2)
We previously disclosed tricylic, 6-carboxylic acid-bearing 4-quinolones as GSK-3β inhibitors. Herein we discuss the optimization of this series to yield a series of more potent 6-nitrile analogs with insignificant anti-microbial activity. Finally,