Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Zuzana Haarhoff"'
Autor:
Matthew D. Hill, Haiquan Fang, Derek Norris, George V. Delucca, Hong Huang, Mikkel DeBenedetto, Claude Quesnelle, William D. Schmitz, John S. Tokarski, Steven Sheriff, Chunhong Yan, Caroline Fanslau, Zuzana Haarhoff, Christine Huang, Melissa Kramer, Shilpa Madari, Krista Menard, Laura Monereau, John Morrison, Nirmala Raghavan, Eric E. Shields, Jean Simmermacher-Mayer, Michael Sinz, Ching Kim Tye, Richard Westhouse, Chunshan Xie, Haiying Zhang, Lisa Zhang, Tatyana Zvyaga, Francis Lee, Ashvinikumar V. Gavai, Andrew P. Degnan
Publikováno v:
ACS Medicinal Chemistry Letters. 13:1165-1171
We describe the synthesis of triazole-containing carboline derivatives and their utility as bromodomain and extra-terminal (BET) inhibitors. A convergent synthetic route permitted the detailed investigation of deuteration and fluorination strategies
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e35ad654e0ca7192653d0e07258cff5
https://doi.org/10.1021/acsmedchemlett.2c00219
https://doi.org/10.1021/acsmedchemlett.2c00219
Autor:
Andrew P. Degnan, Haiquan Fang, Tatyana Zvyaga, Zuzana Haarhoff, Claude A. Quesnelle, Melissa Kramer, Frank Marsilio, Richard A. Westhouse, John S. Tokarski, Shilpa Madari, Jiuqiao Zhao, Amy Wiebesiek, Chunhong Yan, Francis Y. Lee, Michael Sinz, John Morrison, Jean Simmermacher-Mayer, Carolynn Fanslau, Steven Sheriff, Lisa Huang, Ashvinikumar V. Gavai, Chunshan Xie, Matthew D. Hill, Gerry Everlof
Publikováno v:
Bioorganicmedicinal chemistry letters. 51
We describe our efforts to introduce structural diversity to a previously described triazole-containing N1-carboline series of bromodomain and extra-terminal (BET) inhibitors. N9 carbolines were designed to retain favorable binding interactions that
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ada735600c02c9c410a77e52ab96e515
https://pubmed.ncbi.nlm.nih.gov/34560263
https://pubmed.ncbi.nlm.nih.gov/34560263
Autor:
Chunhong Yan, Francis Y. Lee, Ashvinikumar V. Gavai, Melissa Kramer, Frank Marsilio, Eric Shields, Laura Monereau, Zuzana Haarhoff, Richard A. Westhouse, Lisa Zhang, Gerry Everlof, John S. Tokarski, Matthew D. Hill, Tatyana Zvyaga, Asoka Ranasinghe, Carolynn Fanslau, Ching Kim Tye, Steven Sheriff, Christine Huang, Andrew P. Degnan, Krista Menard, John Morrison, Haiquan Fang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 44:128108
We describe our efforts to identify structurally diverse leads in the triazole-containing N1-carboline series of bromodomain and extra-terminal inhibitors. Replacement of the N5 “cap” phenyl moiety with various heteroaryls, coupled with additiona
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6dd1b9be7f6bf8d56a691226fab9f262
https://doi.org/10.1016/j.bmcl.2021.128108
https://doi.org/10.1016/j.bmcl.2021.128108
Autor:
Dawn D. Parker, Karen Rigat, Kyle J. Eastman, Umesh Hanumegowda, Katharine A. Grant-Young, Nicholas A. Meanwell, Maria Tuttle, Tao Wang, Tatyana Zvyaga, Susan B. Roberts, Hua Fang, Kap-Sun Yeung, Mengping Liu, Julie A. Lemm, Kathy Mosure, Xiaoliang Zhuo, Maria Donoso, Kyle Parcella, Zhongxing Zhang, Matthew G. Soars, Zuzana Haarhoff, Zhiwei Yin, Ying-Kai Wang, John F. Kadow, Juliang Zhu
Publikováno v:
ACS Medicinal Chemistry Letters. 8:771-774
Iterative structure–activity analyses in a class of highly functionalized furo[2,3-b]pyridines led to the identification of the second generation pan-genotypic hepatitis C virus NS5B polymerase primer grip inhibitor BMT-052 (14), a potential clinic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::21db76c03898e00a9f3ff613bf9bd713
https://doi.org/10.1021/acsmedchemlett.7b00211
https://doi.org/10.1021/acsmedchemlett.7b00211
Autor:
Dieter M. Drexler, Andrew Dennis Wagner, Zuzana Haarhoff, Pierre Picard, Tatyana Zvyaga, Wilson Z. Shou
Publikováno v:
SLAS Discovery. 21:165-175
The move toward label-free screening in drug discovery has increased the demand for mass spectrometry (MS)-based analysis. Here we investigated the approach of coupling acoustic sample deposition (ASD) with laser diode thermal desorption (LDTD)-tande
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ddb762d7766b87527cef64c9626ae495
https://doi.org/10.1177/1087057115607184
https://doi.org/10.1177/1087057115607184
Autor:
Katharine A. Grant-Young, Maria Tuttle, Nicholas A. Meanwell, Susan B. Roberts, Maria Donoso, Kap-Sun Yeung, Ying-Kai Wang, Matthew G. Soars, Julie A. Lemm, Vivek Halan, Tatyana Zvyaga, Kyle J. Eastman, Jeffrey Tredup, Zuzana Haarhoff, Karen Rigat, Xiaoliang Zhuo, Umesh Hanumegowda, Steven Sheriff, Kathy Mosure, Kaushik Ghosh, Kyle Parcella, Hua Fang, Adam G. Jardel, Brett R. Beno, Kevin Kish, Tao Wang, Dawn D. Parker, Zhiwei Yin, Zhongxing Zhang, John F. Kadow, Juliang Zhu
Publikováno v:
MedChemComm. 8(4)
The development of a series of novel 7-azabenzofurans exhibiting pan-genotype inhibition of HCV NS5B polymerase via binding to the primer grip site is presented. Many challenges, including poor oral bioavailability, high clearance, bioactivation, hig
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::01dcdac30bf36eacc82dc48323620d4b
https://pubmed.ncbi.nlm.nih.gov/30108798
https://pubmed.ncbi.nlm.nih.gov/30108798
Autor:
Murali Subramanian, Tatyana Zvyaga, Jun Zhang, A. David Rodrigues, Zuzana Haarhoff, Priyadeep Bhutani, Melissa A Kramer
Publikováno v:
Xenobiotica; the fate of foreign compounds in biological systems. 47(6)
1. Members of the cytochrome P450 3A (CYP3A) subfamily metabolize numerous compounds and serve as the loci of drug–drug interactions (DDIs). Because of high amino acid sequence identity with human CYP3A, the cynomolgus monkey has been proposed as a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7dbfe5383df34fa000acaa19f551e64e
https://pubmed.ncbi.nlm.nih.gov/27498589
https://pubmed.ncbi.nlm.nih.gov/27498589