Bioorganic and Medicinal Chemistry Letters 
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This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.Discovery of (S)-3-(4-(benzyloxy)phenyl)-2-(2-phenoxyacetamido)propanoic acid derivatives as a new class of GPR34 antagonists
Bioorg Med Chem Lett. 2023 Nov 8:129548. doi: 10.1016/j.bmcl.2023.129548. Online ahead of print.ABSTRACTGPR34 is a rhodopsin-like class G protein-coupled receptor (GPCR) that is involved in the development and progression of several diseases. Despite its importance, effective targeting strategies are lacking. We herein report a series of (S)-3-(4-(benzyloxy)phenyl)-2-(2-phenoxyacetamido)propanoic acid derivatives as a new class of GPR34 antagonists. Structure-activity relationship (SAR) studies led to the identification of the most potent compound, 5e, which displayed an IC50 value of 0.680 μM in the GloSensor cAMP assay ...
Source: Bioorganic and Medicinal Chemistry Letters - November 10, 2023 Category: Chemistry Authors: Pei Zhou Jinlong Zhao Qian Hu Guifeng Lin Jiahao Zhang Anjie Xia Shiyu Zhang Jinshan Nan Linli Li Source Type: research
Discovery of PFI-6, a small-molecule chemical probe for the YEATS domain of MLLT1 and MLLT3
Bioorg Med Chem Lett. 2023 Nov 7:129546. doi: 10.1016/j.bmcl.2023.129546. Online ahead of print.ABSTRACTEpigenetic proteins containing YEATS domains (YD) are an emerging target class in drug discovery. Described herein are the discovery and characterization efforts associated with PFI-6, a new chemical probe for the YD of MLLT1 (ENL/YEATS1) and MLLT3 (AF9/YEATS3). For hit identification, fragment-like mimetics of endogenous YD ligands (crotonylated histone-containing proteins), were synthesized via parallel medicinal chemistry (PMC) and screened for MLLT1 binding. Subsequent SAR studies led to iterative MLLT1/3 binding and...
Source: Bioorganic and Medicinal Chemistry Letters - November 9, 2023 Category: Chemistry Authors: Brigitt Raux Karly A Buchan James Bennett Thomas Christott Matthew S Dowling Gillian Farnie Oleg Fedorov Vicki Gamble Carina Gileadi Charline Giroud Kilian V M Huber Magdalena Korczynska Chris Limberakis Arjun Narayanan Dafydd R Owen Laura D íaz Sáez In Source Type: research
Discovery of 3-oxo-1,2,3,4-tetrahydropyrido[1,2-a]pyrazin derivatives as SARS-CoV-2 main protease inhibitors through virtual screening and biological evaluation
Bioorg Med Chem Lett. 2023 Nov 7:129547. doi: 10.1016/j.bmcl.2023.129547. Online ahead of print.ABSTRACTThe COVID-19 caused by SARS-CoV-2 has led to a global pandemic that continues to impact societies and economies worldwide. The main protease (Mpro) plays a crucial role in SARS-CoV-2 replication and is an attractive target for anti-SARS-CoV-2 drug discovery. Herein, we report a series of 3-oxo-1,2,3,4-tetrahydropyrido[1,2-a]pyrazin derivatives as non-peptidomimetic inhibitors targeting SARS-CoV-2 Mpro through structure-based virtual screening and biological evaluation. Further similarity search and structure-activity rel...
Source: Bioorganic and Medicinal Chemistry Letters - November 9, 2023 Category: Chemistry Authors: Xiaodong Dou Qi Sun Yameng Liu Yangbin Lu Caifang Zhang Guofeng Xu Yue Xu Tongyu Huo Xinyi Zhao Lingyu Su Yihong Xing Luhua Lai Ning Jiao Source Type: research
Discovery of PFI-6, a small-molecule chemical probe for the YEATS domain of MLLT1 and MLLT3
Bioorg Med Chem Lett. 2023 Nov 7:129546. doi: 10.1016/j.bmcl.2023.129546. Online ahead of print.ABSTRACTEpigenetic proteins containing YEATS domains (YD) are an emerging target class in drug discovery. Described herein are the discovery and characterization efforts associated with PFI-6, a new chemical probe for the YD of MLLT1 (ENL/YEATS1) and MLLT3 (AF9/YEATS3). For hit identification, fragment-like mimetics of endogenous YD ligands (crotonylated histone-containing proteins), were synthesized via parallel medicinal chemistry (PMC) and screened for MLLT1 binding. Subsequent SAR studies led to iterative MLLT1/3 binding and...
Source: Bioorganic and Medicinal Chemistry Letters - November 9, 2023 Category: Chemistry Authors: Brigitt Raux Karly A Buchan James Bennett Thomas Christott Matthew S Dowling Gillian Farnie Oleg Fedorov Vicki Gamble Carina Gileadi Charline Giroud Kilian V M Huber Magdalena Korczynska Chris Limberakis Arjun Narayanan Dafydd R Owen Laura D íaz Sáez In Source Type: research
Discovery of 3-oxo-1,2,3,4-tetrahydropyrido[1,2-a]pyrazin derivatives as SARS-CoV-2 main protease inhibitors through virtual screening and biological evaluation
Bioorg Med Chem Lett. 2023 Nov 7:129547. doi: 10.1016/j.bmcl.2023.129547. Online ahead of print.ABSTRACTThe COVID-19 caused by SARS-CoV-2 has led to a global pandemic that continues to impact societies and economies worldwide. The main protease (Mpro) plays a crucial role in SARS-CoV-2 replication and is an attractive target for anti-SARS-CoV-2 drug discovery. Herein, we report a series of 3-oxo-1,2,3,4-tetrahydropyrido[1,2-a]pyrazin derivatives as non-peptidomimetic inhibitors targeting SARS-CoV-2 Mpro through structure-based virtual screening and biological evaluation. Further similarity search and structure-activity rel...
Source: Bioorganic and Medicinal Chemistry Letters - November 9, 2023 Category: Chemistry Authors: Xiaodong Dou Qi Sun Yameng Liu Yangbin Lu Caifang Zhang Guofeng Xu Yue Xu Tongyu Huo Xinyi Zhao Lingyu Su Yihong Xing Luhua Lai Ning Jiao Source Type: research
