Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Yong L. Zhu"'
Autor:
John P. Anderson, Dean R. Artis, Hing L. Sham, Roy K. Hom, Michael S. Dappen, Andrei W. Konradi, Simeon Bowers, Hu Pan, Robert A. Galemmo, Marc Adler, Pearl Tanaka, May Lin, Jeanne Baker, Lany Ruslim, Donald J. Fauss, Zhao Ren, Yong L. Zhu, Anh P. Truong, Danny Tam, Marcelle Bergeron, Lee H. Latimer, Paul Beroza, Jacek Jagodzinski, Heather Zhang, Michael P. Bova, George Tonn, Linnea Diep, Ruth Motter, Kent Fitzgerald, Nanhua Yao, Wayman Chan, Jennifer K. Hoffman, R. Jeffrey Neitz, Danielle L. Aubele
Publikováno v:
ChemMedChem. 8:1295-1313
Polo-like kinase-2 (Plk-2) has been implicated as the dominant kinase involved in the phosphorylation of α-synuclein in Lewy bodies, which are one of the hallmarks of Parkinson's disease neuropathology. Potent, selective, brain-penetrant inhibitors
Autor:
Yong L. Zhu, Krishnamurthy Shyam, Philip G. Penketh, Kimiko Ishiguro, Alan C. Sartorelli, Raymond P. Baumann
Publikováno v:
Biochemical Pharmacology. 79:1553-1561
1,2-Bis(methylsulfonyl)-1-(2-chloroethyl)-2-[[1-(4-nitrophenyl)ethoxy]carbonyl]hydrazine (KS119) is a prodrug of the 1,2-bis(sulfonyl)hydrazine class of antineoplastic agents designed to exploit the oxygen-deficient regions of cancerous tissue. Thus,
Autor:
Hing L. Sham, Ying-Zi Xu, Zhao Ren, Shendong Yuan, Julie Lougheed, Eric Brecht, Wayman Chan, Roy K. Hom, Lany Ruslim, Paul Beroza, Michael P. Bova, Dean R. Artis, Yong L. Zhu, Jiangli Yan, Simeon Bowers, Danny Tam, Hu Pan, Nanhua Yao
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(10)
Utilizing a structure based design approach, combined with extensive medicinal chemistry execution, highly selective, potent and novel BACE1 inhibitor 8 (BACE1 Alpha assay IC50=8nM) was made from a weak μM potency hit in an extremely efficient way.
Autor:
Paul Beroza, Michael P. Bova, Jennifer K. Hoffman, Jennifer Sealy, Heather Zhang, Marcelle Bergeron, Linnea Diep, Danny Tam, Ruth Motter, Zhao Ren, R. Jeffrey Neitz, Danielle L. Aubele, Kent Fitzgerald, Michael Ye, Wayman Chan, Pearl Tanaka, Deepal Pandya, Donald J. Fauss, Andrei W. Konradi, John P. Anderson, Roy K. Hom, Dean R. Artis, Hing L. Sham, Robert A. Galemmo, George Tonn, Jeanne Baker, Lany Ruslim, Yong L. Zhu, Anh P. Truong, Michael S. Dappen, Simeon Bowers
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(9)
Polo-like kinase-2 (Plk-2) is a potential therapeutic target for Parkinson’s disease and this Letter describes the SAR of a series of dihydropteridinone based Plk-2 inhibitors. By optimizing both the N-8 substituent and the biaryl region of the inh
Autor:
Gary Probst, Nanhua Yao, Danny Tam, Julie Lougheed, Zhao Ren, Hu Pan, Ying-Zi Xu, Wayman Chan, Dean R. Artis, Lany Ruslim, Shendong Yuan, Roy K. Hom, Yong L. Zhu, Paul Beroza, Andrei W. Konradi, Eric Brecht, Michael P. Bova, Hing L. Sham, Simeon Bowers
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(7)
The structure–activity relationship of a series of dihydroisoquinoline BACE-1 inhibitors is described. Application of structure-based design to screening hit 1 yielded sub-micromolar inhibitors. Replacement of the carboxylic acid of 1 was guided by