Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Neil H. Squires"'
Autor:
Todd Appleby, Martijn Fenaux, Thomas Butler, Mark Charles Whitcomb, Gregory Chin, Rick Lee, Gabriel Birkus, Aesop Cho, Michael O'neil Hanrahan Clarke, Thorsten A. Kirschberg, Darius Babusis, Vangelis Aktoudianakis, Lijun Zhang, Thomas E. Edwards, Eisuke Murakami, Jie Xu, Choung U. Kim, Daniel Byun, Neil H. Squires, Edward Doerffler, Willard Lew, Adrian S. Ray, Joy Y. Feng, Ona Barauskas, Sammy Metobo, Ting Wang, Huiling Yang, Yeojin Park, Mish Michael R, Neeraj Tirunagari, Hong Ye
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:1840-1847
A series of 2′-fluorinated C -nucleosides were prepared and tested for anti-HCV activity. Among them, the triphosphate of 2′-fluoro-2′- C -methyl adenosine C -nucleoside ( 15 ) was a potent and selective inhibitor of the NS5B polymerase and mai
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c64ac988d715937da5d9882b1446f78
https://doi.org/10.1016/j.bmcl.2017.02.037
https://doi.org/10.1016/j.bmcl.2017.02.037
Autor:
Choung U. Kim, Lijun Zhang, Ke-Yu Wang, Adrian S. Ray, Mish Michael R, Aesop Cho, Martijn Fenaux, Yeojin Park, Darius Babusis, Joy Y. Feng, Thorsten A. Kirschberg, Neil H. Squires
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1040-1043
The first synthesis of 1'-C-CN, 2'-F, 2'-C-Me pyrimidines is described. Anti-HCV activity was assessed and compared to the 1'-C-CN, 2'-C-Me as well as the 2'-F, 2'-C-Me pyrimidines. A phosphoramidate prodrug of the cytidine derivative showed activity
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e929ee839d0aa724863d04acd3ded658
https://doi.org/10.1016/j.bmcl.2015.01.021
https://doi.org/10.1016/j.bmcl.2015.01.021
Autor:
Huiling Yang, X. Christopher Sheng, Neeraj Tirunagari, Choung U. Kim, Thorsten A. Kirschberg, Amoreena C. Corsa, Neil H. Squires, Yang Tian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:969-972
A sulfonamide replacement of the P2–P3 amide bond in the context of macrocyclic HCV NS3 protease inhibitors was investigated. These analogs displayed good inhibitory potency in the absence of any P3 capping group. The synthesis and preliminary SAR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::94f6c6f845ab359f3e2bb10394090be0
https://doi.org/10.1016/j.bmcl.2013.12.060
https://doi.org/10.1016/j.bmcl.2013.12.060
Autor:
Kelly Wang, James G. Taylor, Elsa Mondou, Mike Matles, Yang Zheng-Yu, Yujin Wang, Hongtao Liu, Jianyu Sun, Yang Tian, Guofeng Cheng, Hongyan Guo, Lianhong Xu, Melanie Cornpropst, Jason K. Perry, Michael L. Mitchell, Thorsten Kirschberg, Kato Darryl, Manoj C. Desai, Chris Yang, Neil H. Squires, John O. Link, Terry Kellar, Erik Mogalian, Jay P. Parrish
Publikováno v:
Journal of Medicinal Chemistry. 57:2033-2046
A new class of highly potent NS5A inhibitors with an unsymmetric benzimidazole-difluorofluorene-imidazole core and distal [2.2.1]azabicyclic ring system was discovered. Optimization of antiviral potency and pharmacokinetics led to the identification
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e01a36ec6ef38fbdea906289d7749e6
https://doi.org/10.1021/jm401499g
https://doi.org/10.1021/jm401499g
Autor:
Rebecca Hluhanich, Eric B. Lansdon, Neil H. Squires, Mini Balakrishnan, Thorsten A. Kirschberg, Wei Huang, Nilima Kutty, Albert Liclican, Damian J. McColl
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1131-1134
A series of 3,4,5-trisubstituted 1,2,4-4H triazole derivatives was synthesized and investigated for HIV-1 reverse transcriptase inhibition. An X-ray structure with HIV-1 RT secured the binding mode and allowed the key interactions with the enzyme to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d7a170eed305b2d2c0ff050038ac540
https://doi.org/10.1016/j.bmcl.2007.11.127
https://doi.org/10.1016/j.bmcl.2007.11.127
Autor:
Juthamas Sukbuntherng, Catherine Magill, John Eksterowicz, Doris Graupe, Michael J. Green, Penglie Zhang, Hyunjin M. Kim, Martin Sendzik, Peter Sabbatini, Jason Oeh, Jeffrey R. Spencer, Stacie A. Dalrymple, Peter R. Young, Katherine G. Moss, Andrew G. Myers, Neil H. Squires
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4884-4888
Novel analogs of (-)-saframycin A are described. The analogs are shown to be potent inhibitors of the in vitro growth of several tumor cells in a broad panel and promising as leads for further optimization. The first in vivo studies in a solid tumor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::211f339c2f46146df07ee8a6fabe3a5f
https://doi.org/10.1016/j.bmcl.2006.06.085
https://doi.org/10.1016/j.bmcl.2006.06.085
Autor:
Bradley A. Katz, Danny McGee, Martin Sendzik, Christine Luong, Richard L. Mackman, Jeffrey R. Spencer, Allen Darin Arthur, Neil H. Squires
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:2023-2026
The structure-based design of potent and selective urokinase-type plasminogen activator (uPA) inhibitors with 4-aminoarylamidine or 4-aminoarylguanidine S1 binding groups, is described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37e511779851ef634ec4a86932cdff4a
https://doi.org/10.1016/s0960-894x(02)00312-8
https://doi.org/10.1016/s0960-894x(02)00312-8
Autor:
Mini Balakrishnan, Katherine M. Brendza, Michael Wang, Eugene J. Eisenberg, Thorsten A. Kirschberg, Jason K. Perry, Nilima Kutty, Xiaohong Liu, Tiffany Barnes, Xiaowu Chen, Eric B. Lansdon, Weili Jin, Stephanie A. Leavitt, William J. Watkins, John Mak, Liu Qi, Albert Liclican, Neil H. Squires
Publikováno v:
Journal of medicinal chemistry. 52(19)
Pyrimidinol carboxylic acids were designed as inhibitors of HIV-1 RNase H function. These molecules can coordinate to two divalent metal ions in the RNase H active site. Inhibition of enzymatic activity was measured in a biochemical assay, but no ant
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::479c6945f71b1528c1886e9bf7f0f317
https://pubmed.ncbi.nlm.nih.gov/19791799
https://pubmed.ncbi.nlm.nih.gov/19791799
Autor:
Catherine Magill, Lee Honigberg, Ronnel Cabuslay, Neil H. Squires, Nancy Waldeck, James W. Janc, Martin Sendzik, Richard L. Mackman
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(12)
The rational design and synthesis of beta-amino-alpha-hydroxy amide derivatives as reversible inhibitors of methionine aminopeptidase-2 (MetAP2) with anti-proliferative activity against human umbilical vein endothelial cells (HUVECs) is described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3432cd9d3d05eaf37bd2a03cec23348f
https://pubmed.ncbi.nlm.nih.gov/15149671
https://pubmed.ncbi.nlm.nih.gov/15149671
Autor:
Thorsten A. Kirschberg, Mini Balakrishnan, Neil H. Squires, Tiffany Barnes, Katherine M. Brendza, Xiaowu Chen, Eugene J. Eisenberg, Weili Jin, Nilima Kutty, Stephanie Leavitt, Albert Liclican, Qi Liu, Xiaohong Liu, John Mak, Jason K. Perry, Michael Wang, William J. Watkins, Eric B. Lansdon
Publikováno v:
Journal of Medicinal Chemistry; Oct2009, Vol. 52 Issue 19, p5781-5784, 4p