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Design and optimization of piperlongumine analogs as potent senolytics
In this study, our medicinal chemistry campaign on both the α,β-unsaturated δ-valerolactam ring and the phenyl ring of PL culminated in the identification of compound 24, which exhibited an impressive 50-fold enhancement in senolytic activity against senescent WI-38 fibroblasts compared to PL.PMID:38104906 | DOI:10.1016/j.bmcl.2023.129593 (Source: Bioorganic and Medicinal Chemistry Letters)
Source: Bioorganic and Medicinal Chemistry Letters - December 17, 2023 Category: Chemistry Authors: Xuan Zhang Yonghan He Xingui Liu Xin Zhang Peizhong Shi Yingying Wang Daohong Zhou Guangrong Zheng Source Type: research

Truncated derivatives of amphidinol 3 reveal the functional role of polyol chain in sterol-recognition and pore formation
Bioorg Med Chem Lett. 2023 Dec 15;98:129594. doi: 10.1016/j.bmcl.2023.129594. Online ahead of print.ABSTRACTHere we examined the membrane binding and pore formation of amphidinol 3 (AM3) and its truncated synthetic derivatives. Importantly, both of the membrane affinity and pore formation activity were well correlated with the reported antifungal activity. Our data clearly demonstrated that the C1-C30 moiety of AM3 plays essential roles both in sterol recognition and stable pore formation. Based on the current findings, we updated the interacting model between AM3 and sterol, in which the moiety encompassing from C21 to C6...
Source: Bioorganic and Medicinal Chemistry Letters - December 17, 2023 Category: Chemistry Authors: Nobuaki Matsumori Manami Hieda Masayuki Morito Yuma Wakamiya Tohru Oishi Source Type: research

Design and optimization of piperlongumine analogs as potent senolytics
In this study, our medicinal chemistry campaign on both the α,β-unsaturated δ-valerolactam ring and the phenyl ring of PL culminated in the identification of compound 24, which exhibited an impressive 50-fold enhancement in senolytic activity against senescent WI-38 fibroblasts compared to PL.PMID:38104906 | DOI:10.1016/j.bmcl.2023.129593 (Source: Bioorganic and Medicinal Chemistry Letters)
Source: Bioorganic and Medicinal Chemistry Letters - December 17, 2023 Category: Chemistry Authors: Xuan Zhang Yonghan He Xingui Liu Xin Zhang Peizhong Shi Yingying Wang Daohong Zhou Guangrong Zheng Source Type: research

Truncated derivatives of amphidinol 3 reveal the functional role of polyol chain in sterol-recognition and pore formation
Bioorg Med Chem Lett. 2023 Dec 15;98:129594. doi: 10.1016/j.bmcl.2023.129594. Online ahead of print.ABSTRACTHere we examined the membrane binding and pore formation of amphidinol 3 (AM3) and its truncated synthetic derivatives. Importantly, both of the membrane affinity and pore formation activity were well correlated with the reported antifungal activity. Our data clearly demonstrated that the C1-C30 moiety of AM3 plays essential roles both in sterol recognition and stable pore formation. Based on the current findings, we updated the interacting model between AM3 and sterol, in which the moiety encompassing from C21 to C6...
Source: Bioorganic and Medicinal Chemistry Letters - December 17, 2023 Category: Chemistry Authors: Nobuaki Matsumori Manami Hieda Masayuki Morito Yuma Wakamiya Tohru Oishi Source Type: research

Design and Optimization of Piperlongumine Analogs as Potent Senolytics
In this study, our medicinal chemistry campaign on both the α,β-unsaturated δ-valerolactam ring and the phenyl ring of PL culminated in the identification of compound 24, which exhibited an impressive 50-fold enhancement in senolytic activity against senescent WI-38 fibroblasts compared to PL.PMID:38104906 | DOI:10.1016/j.bmcl.2023.129593 (Source: Bioorganic and Medicinal Chemistry Letters)
Source: Bioorganic and Medicinal Chemistry Letters - December 17, 2023 Category: Chemistry Authors: Xuan Zhang Yonghan He Xingui Liu Xin Zhang Peizhong Shi Yingying Wang Daohong Zhou Guangrong Zheng Source Type: research

Truncated derivatives of amphidinol 3 reveal the functional role of polyol chain in sterol-recognition and pore formation
Bioorg Med Chem Lett. 2023 Dec 15:129594. doi: 10.1016/j.bmcl.2023.129594. Online ahead of print.ABSTRACTHere we examined the membrane binding and pore formation of amphidinol 3 (AM3) and its truncated synthetic derivatives. Importantly, both of the membrane affinity and pore formation activity were well correlated with the reported antifungal activity. Our data clearly demonstrated that the C1-C30 moiety of AM3 plays essential roles both in sterol recognition and stable pore formation. Based on the current findings, we updated the interacting model between AM3 and sterol, in which the moiety encompassing from C21 to C67 a...
Source: Bioorganic and Medicinal Chemistry Letters - December 17, 2023 Category: Chemistry Authors: Nobuaki Matsumori Manami Hieda Masayuki Morito Yuma Wakamiya Tohru Oishi Source Type: research

Design and Optimization of Piperlongumine Analogs as Potent Senolytics
In this study, our medicinal chemistry campaign on both the α,β-unsaturated δ-valerolactam ring and the phenyl ring of PL culminated in the identification of compound 24, which exhibited an impressive 50-fold enhancement in senolytic activity against senescent WI-38 fibroblasts compared to PL.PMID:38104906 | DOI:10.1016/j.bmcl.2023.129593 (Source: Bioorganic and Medicinal Chemistry Letters)
Source: Bioorganic and Medicinal Chemistry Letters - December 17, 2023 Category: Chemistry Authors: Xuan Zhang Yonghan He Xingui Liu Xin Zhang Peizhong Shi Yingying Wang Daohong Zhou Guangrong Zheng Source Type: research

Truncated derivatives of amphidinol 3 reveal the functional role of polyol chain in sterol-recognition and pore formation
Bioorg Med Chem Lett. 2023 Dec 15:129594. doi: 10.1016/j.bmcl.2023.129594. Online ahead of print.ABSTRACTHere we examined the membrane binding and pore formation of amphidinol 3 (AM3) and its truncated synthetic derivatives. Importantly, both of the membrane affinity and pore formation activity were well correlated with the reported antifungal activity. Our data clearly demonstrated that the C1-C30 moiety of AM3 plays essential roles both in sterol recognition and stable pore formation. Based on the current findings, we updated the interacting model between AM3 and sterol, in which the moiety encompassing from C21 to C67 a...
Source: Bioorganic and Medicinal Chemistry Letters - December 17, 2023 Category: Chemistry Authors: Nobuaki Matsumori Manami Hieda Masayuki Morito Yuma Wakamiya Tohru Oishi Source Type: research

Design and Optimization of Piperlongumine Analogs as Potent Senolytics
In this study, our medicinal chemistry campaign on both the α,β-unsaturated δ-valerolactam ring and the phenyl ring of PL culminated in the identification of compound 24, which exhibited an impressive 50-fold enhancement in senolytic activity against senescent WI-38 fibroblasts compared to PL.PMID:38104906 | DOI:10.1016/j.bmcl.2023.129593 (Source: Bioorganic and Medicinal Chemistry Letters)
Source: Bioorganic and Medicinal Chemistry Letters - December 17, 2023 Category: Chemistry Authors: Xuan Zhang Yonghan He Xingui Liu Xin Zhang Peizhong Shi Yingying Wang Daohong Zhou Guangrong Zheng Source Type: research

Synthesis, antibiofilm activity and molecular docking of N-acylhomoserine lactones containing cinammic moieties
Bioorg Med Chem Lett. 2023 Dec 13;98:129592. doi: 10.1016/j.bmcl.2023.129592. Online ahead of print.ABSTRACTWe prepared a series of cinnamoyl-containing furanones by an affordable and short synthesis. The nineteen compounds hold a variety of substituents including electron-donating, electron-withdrawing, bulky and meta-substituted phenyls, as well as heterocyclic rings. Compounds showed antibiofilm activity in S. aureus, K. pneumoniae and, more pronounced, against P. aeruginosa. The disruption of quorum sensing (QS) was tested using the violacein test and molecular docking predicted the antagonism of LasR as a plausible me...
Source: Bioorganic and Medicinal Chemistry Letters - December 15, 2023 Category: Chemistry Authors: Ángel Ramírez-Trinidad Ernesto Mart ínez-Solano C ésar E Tovar-Roman Mariana Garc ía-Guerrero Jos é A Rivera-Chávez Eduardo Hern ández-Vázquez Source Type: research

Synthesis, antibiofilm activity and molecular docking of N-acylhomoserine lactones containing cinammic moieties
Bioorg Med Chem Lett. 2023 Dec 13:129592. doi: 10.1016/j.bmcl.2023.129592. Online ahead of print.ABSTRACTWe prepared a series of cinnamoyl-containing furanones by an affordable and short synthesis. The nineteen compounds hold a variety of substituents including electron-donating, electron-withdrawing, bulky and meta-substituted phenyls, as well as heterocyclic rings. Compounds showed antibiofilm activity in S. aureus, K. pneumoniae and, more pronounced, against P. aeruginosa. The disruption of quorum sensing (QS) was tested using the violacein test and molecular docking predicted the antagonism of LasR as a plausible mecha...
Source: Bioorganic and Medicinal Chemistry Letters - December 15, 2023 Category: Chemistry Authors: Ángel Ramírez-Trinidad Ernesto Mart ínez-Solano C ésar E Tovar-Roman Mariana Garc ía-Guerrero Jos é A Rivera-Chávez Eduardo Hern ández-Vázquez Source Type: research

Exploration of macrocyclic peptide binders to the extracellular CRD domain of human receptor tyrosine kinase-like orphan receptor 1 (ROR1)
Bioorg Med Chem Lett. 2023 Dec 12:129589. doi: 10.1016/j.bmcl.2023.129589. Online ahead of print.ABSTRACTElevated levels of receptor tyrosine kinase-like orphan receptor 1 (RORl) expression are observed in multiple hematological and solid tumors, but not in most of the healthy adult tissues, identifying ROR1 as an attractive target for tumor-specific therapy. Herein we will describe the discovery of macrocyclic peptides as binders of the extracellular Cysteine-Rich Domain (CRD) of human ROR1 via mRNA in vitro selection technology using the PDPS platform, followed by exploration of sidechain SAR of parent macrocycle peptide...
Source: Bioorganic and Medicinal Chemistry Letters - December 14, 2023 Category: Chemistry Authors: Jennifer X Qiao Mark R Witmer Ving Lee Tammy C Wang Patrick C Reid Yuki Arioka Glen Farr Melissa Hill-Drzewi Liang Schweizer Aaron Yamniuk Lin Cheng Bozena Abramczyk Martin Corbett Deepa Calambur Nicolas Szapiel Rolf Ryseck Paul Ponath Michael A Poss Perc Source Type: research

Design, Synthesis, and Biological Evaluation of Novel 8-Substituted Quercetin Derivatives Targeting the β‑Catenin/B-Cell Lymphoma 9 Interaction
Bioorg Med Chem Lett. 2023 Dec 12:129591. doi: 10.1016/j.bmcl.2023.129591. Online ahead of print.ABSTRACTThe β-catenin/B-cell lymphoma 9 (BCL9) protein-protein interaction (PPI) is a potential target for aberrantly active Wnt/β-catenin signaling which actively participates in initiating and progressing of many cancers. Herein, we discovered novel 8-substituted quercetin derivatives with potential inhibitory activities targeting β-catenin/BCL9 PPI. Among all the derivatives, compound B4 displayed the most promising PPI inhibitory activity with an IC50 value of 2.25 μM in a competitive fluorescence polarization assay and...
Source: Bioorganic and Medicinal Chemistry Letters - December 14, 2023 Category: Chemistry Authors: Xinyan Peng Li-An Shen Ya Bao Chenglong Liu Qiushi Chen Hao Zhang Jiayi Li Qingwei Zhang Source Type: research

Exploration of macrocyclic peptide binders to the extracellular CRD domain of human receptor tyrosine kinase-like orphan receptor 1 (ROR1)
Bioorg Med Chem Lett. 2023 Dec 12:129589. doi: 10.1016/j.bmcl.2023.129589. Online ahead of print.ABSTRACTElevated levels of receptor tyrosine kinase-like orphan receptor 1 (RORl) expression are observed in multiple hematological and solid tumors, but not in most of the healthy adult tissues, identifying ROR1 as an attractive target for tumor-specific therapy. Herein we will describe the discovery of macrocyclic peptides as binders of the extracellular Cysteine-Rich Domain (CRD) of human ROR1 via mRNA in vitro selection technology using the PDPS platform, followed by exploration of sidechain SAR of parent macrocycle peptide...
Source: Bioorganic and Medicinal Chemistry Letters - December 14, 2023 Category: Chemistry Authors: Jennifer X Qiao Mark R Witmer Ving Lee Tammy C Wang Patrick C Reid Yuki Arioka Glen Farr Melissa Hill-Drzewi Liang Schweizer Aaron Yamniuk Lin Cheng Bozena Abramczyk Martin Corbett Deepa Calambur Nicolas Szapiel Rolf Ryseck Paul Ponath Michael A Poss Perc Source Type: research

Design, Synthesis, and Biological Evaluation of Novel 8-Substituted Quercetin Derivatives Targeting the β‑Catenin/B-Cell Lymphoma 9 Interaction
Bioorg Med Chem Lett. 2023 Dec 12:129591. doi: 10.1016/j.bmcl.2023.129591. Online ahead of print.ABSTRACTThe β-catenin/B-cell lymphoma 9 (BCL9) protein-protein interaction (PPI) is a potential target for aberrantly active Wnt/β-catenin signaling which actively participates in initiating and progressing of many cancers. Herein, we discovered novel 8-substituted quercetin derivatives with potential inhibitory activities targeting β-catenin/BCL9 PPI. Among all the derivatives, compound B4 displayed the most promising PPI inhibitory activity with an IC50 value of 2.25 μM in a competitive fluorescence polarization assay and...
Source: Bioorganic and Medicinal Chemistry Letters - December 14, 2023 Category: Chemistry Authors: Xinyan Peng Li-An Shen Ya Bao Chenglong Liu Qiushi Chen Hao Zhang Jiayi Li Qingwei Zhang Source Type: research