Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Hnin Hnin Khine"'
Autor:
Andre White, Joseph R. Woska, Ho Yin Lo, Josephine King, John P. Wolak, Mohammed A. Kashem, Jörg Bentzien, Hnin Hnin Khine, Roman Wolfgang Fleck, Steven S. Pullen, Chuk Chui Man, Gregory P. Roth, Hidenori Takahashi
Publikováno v:
Tetrahedron Letters. 49:7337-7340
Based on information from molecular modeling, a series of 2-aminobenzimidazoles with pyrrole moieties were designed and synthesized as ITK antagonists. Results showed that a significant improvement of intrinsic and cell-based potency was achieved. X-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0bf5c55c7c49b4297d1b889eb3578745
https://doi.org/10.1016/j.tetlet.2008.10.057
https://doi.org/10.1016/j.tetlet.2008.10.057
Autor:
Michael P. Winters, Renee L. DesJarlais, Mark Bobko, John P. Wolak, Ho Yin Lo, Steven S. Pullen, Deborah D. Jeanfavre, Hnin Hnin Khine, Rosemarie H. Sallati, Ernest L. Raymond, Mohammed A. Kashem, Lei Qiao, Gregory P. Roth, Declan Ryan, Joseph R. Woska, Kevin J. Moriarty, Darius Robinson, Hidenori Takahashi, B. Tomczuk, Wilson Matthew Allan, Ronald L. Magolda, Peter Allen Nemoto, Andre White, Brian Nicholas Cook
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5545-5549
A series of novel potent benzimidazole based inhibitors of interleukin-2 T-cell kinase (Itk) were prepared. In this report, we discuss the structure-activity relationship (SAR), selectivity, and cell-based activity for the series. We also discuss the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77216c0a135ce0c04945949b146cd09c
https://doi.org/10.1016/j.bmcl.2008.09.015
https://doi.org/10.1016/j.bmcl.2008.09.015
Autor:
Stanley Kugler, Mohammed A. Kashem, Ernest L. Raymond, Hidenori Takahashi, Steven S. Pullen, Leslie Martin, Gabriel Labissiere, Jennifer Ahlberg, Jennifer A. Kowalski, Hnin Hnin Khine, Joseph R. Woska, Stéphane De Lombaert, Donna Skow, David S. Thomson, Kathy O’Shea, Brian Nicholas Cook, Renee Zindell, Deborah D. Jeanfavre, Doris Riether, Jörg Bentzien, Kerry L. M. Ralph, Rosemarie Sellati
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(6)
Benzamide 1 demonstrated good potency as a selective ITK inhibitor, however the amide moiety was found to be hydrolytically labile in vivo, resulting in low oral exposure and the generation of mutagenic aromatic amine metabolites. Replacing the benza
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a1df8326828e0236a2add4a210c4153e
https://pubmed.ncbi.nlm.nih.gov/19246196
https://pubmed.ncbi.nlm.nih.gov/19246196
Autor:
John P. Wolak, Ji Wang, Hnin Hnin Khine, Peter Allen Nemoto, Chuk Chui Man, Stéphane De Lombaert, Steven S. Pullen, Hidenori Takahashi, Brian Nicholas Cook, Mohammed A. Kashem, Jörg Bentzien, Andre White, Gregory P. Roth, Fariba Soleymanzadeh, Stanley Kugler
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(3)
Interleukin-2 inducible T-cell kinase (ITK) is a member of the Tec kinase family and is involved with T-cell activation and proliferation. Due to its critical role in acting as a modulator of T-cells, ITK inhibitors could provide a novel route to ant
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fe75d81be2fbcce7cd52565bd9aa148
https://pubmed.ncbi.nlm.nih.gov/19111460
https://pubmed.ncbi.nlm.nih.gov/19111460
Autor:
Jörg Bentzien, Ho Yin Lo, Stanley Kugler, Roman Wolfgang Fleck, Hnin Hnin Khine, Joseph R. Woska, Steven S. Pullen, Mohammed A. Kashem, Hidenori Takahashi
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(23)
Based on the information from molecular modeling and X-ray crystal structures, the kinase specificity pocket of ITK could be occupied upon extension of the right-hand-side of the 2-benzimidazole core of the inhibitors. 2-Aminobenzimidazoles with a tr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a0fafdbfc7ec0a72366c67c251038a8
https://pubmed.ncbi.nlm.nih.gov/18930400
https://pubmed.ncbi.nlm.nih.gov/18930400
Autor:
Gregory P. Roth, Hidenori Takahashi, Hnin Hnin Khine, Steven S. Pullen, Darius Robinson, Declan Ryan, Michael P. Winters, Lei Qiao, Lisa H. Liu, Ronald L. Magolda, Renee DesJarlis, Thomas M. Farrell, Paul Kaplita, Brian Nicholas Cook, Kevin J. Moriarty, Josephine King, Mohammed A. Kashem
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(20)
Previously, we reported a series of novel benzimidazole based Itk inhibitors that exhibited excellent enzymatic potency and selectivity but low microsomal stability. Employing a structure based approach a new series of inhibitors with comparable pote
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::534098900d4e651ba83b91c4680d01bb
https://pubmed.ncbi.nlm.nih.gov/18819794
https://pubmed.ncbi.nlm.nih.gov/18819794
Autor:
Michael P. Winters, Renee L. DesJarlais, Paul Kaplita, Hnin Hnin Khine, Kevin J. Moriarty, Steven S. Pullen, Ernest L. Raymond, Roger J. Snow, Rosemarie Sellati, Gregory P. Roth, Charles L. Cywin, Thomas M. Farrell, Lisa H. Liu, Mohammed A. Kashem, Hidenori Takahashi, Darius Robinson, Joseph R. Woska, Josephine King, John P. Wolak
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(20)
A series of novel 5-aminomethyl-1H-benzimidazole based inhibitors of Itk were prepared. Structure–activity relationships, selectivity and cell activity are reported for this series. Compound 2, a potent and selective antagonist of Itk, inhibited an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::18f86ef5f6bfbacbc788381beadc24eb
https://pubmed.ncbi.nlm.nih.gov/18823779
https://pubmed.ncbi.nlm.nih.gov/18823779
Autor:
Hnin Hnin Khine, Christopher Ronald Sarko, Mohammed A. Kashem, Noel S. Wilson, John P. Wolak, Josephine King, Teresa Roma, Charles L. Cywin, Jennifer A. Kowalski, Scot Campbell, John Lord, Steven S. Pullen, Michael P. Winters, Gregory P. Roth, Asitha Abeywardane, Roger J. Snow
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(13)
Benzimidazole 1 was identified as a selective inhibitor of ITK by high throughput screening. Hit-to-lead studies defined the SAR at all three substituents. Reversing the amide linkage at C6 led to 16, with a fivefold improvement of potency. This enha
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3017ea619ea79276e05159f9c76588ec
https://pubmed.ncbi.nlm.nih.gov/17499505
https://pubmed.ncbi.nlm.nih.gov/17499505
Autor:
John P. Wolak, Brian Nicholas Cook, Andre White, Ronald L. Magolda, Declan Ryan, Deborah D. Jeanfavre, Rosemarie H. Sallati, Gregory Roth, Lei Qiao, Darius Robinson, Wilson Matthew Allan, Ernest L. Raymond, Peter Allen Nemoto, Steven S. Pullen, Joseph R. Woska, Ho Yin Lo, Bruce E. Tomczuk, Hnin Hnin Khine, Mark A. Bobko, Michael P. Winters, Kevin J. Moriarty, Renee L. DesJarlais, Mohammed A. Kashem, Hidenori Takahashi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1835
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7a5b96b24d26df2b34f888a499446a2b
https://doi.org/10.1016/j.bmcl.2008.09.114
https://doi.org/10.1016/j.bmcl.2008.09.114