Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors
In the last decades, inhibitors of histone deacetylases (HDAC) have become an important class of anti-cancer agents. In a previous study we described the synthesis of spiro[chromane-2,4′-piperidine]hydroxamic acid derivatives able to inhibit histone deacetylase enzymes. Herein, we present our explor...
Ausführliche Beschreibung
Gespeichert in:
| Autor*in: |
Thaler, Florian [verfasserIn] |
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| Format: |
E-Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
2016 |
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| Schlagwörter: |
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| Umfang: |
15 |
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| Übergeordnetes Werk: |
Enthalten in: Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles - Jose, Ajay ELSEVIER, 2018, Amsterdam [u.a.] |
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| Übergeordnetes Werk: |
volume:108 ; year:2016 ; day:27 ; month:01 ; pages:53-67 ; extent:15 |
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| DOI / URN: |
10.1016/j.ejmech.2015.11.010 |
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| 520 | |a In the last decades, inhibitors of histone deacetylases (HDAC) have become an important class of anti-cancer agents. In a previous study we described the synthesis of spiro[chromane-2,4′-piperidine]hydroxamic acid derivatives able to inhibit histone deacetylase enzymes. Herein, we present our exploration for new derivatives by replacing the piperidine moiety with various cycloamines. The goal was to obtain highly potent compounds with a good in vitro ADME profile. In addition, molecular modeling studies unravelled the binding mode of these inhibitors. | ||
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10.1016/j.ejmech.2015.11.010 doi GBVA2016008000030.pica (DE-627)ELV019300549 (ELSEVIER)S0223-5234(15)30347-0 DE-627 ger DE-627 rakwb eng 610 610 DE-600 570 540 VZ BIODIV DE-30 fid 42.00 bkl Thaler, Florian verfasserin aut Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors 2016 15 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier In the last decades, inhibitors of histone deacetylases (HDAC) have become an important class of anti-cancer agents. In a previous study we described the synthesis of spiro[chromane-2,4′-piperidine]hydroxamic acid derivatives able to inhibit histone deacetylase enzymes. Herein, we present our exploration for new derivatives by replacing the piperidine moiety with various cycloamines. The goal was to obtain highly potent compounds with a good in vitro ADME profile. In addition, molecular modeling studies unravelled the binding mode of these inhibitors. Antiproliferation Elsevier Molecular modeling Elsevier Epigenetics Elsevier Privileged structures Elsevier Histone deacetylases Elsevier Moretti, Loris oth Amici, Raffaella oth Abate, Agnese oth Colombo, Andrea oth Carenzi, Giacomo oth Fulco, Maria Carmela oth Boggio, Roberto oth Dondio, Giulio oth Gagliardi, Stefania oth Minucci, Saverio oth Sartori, Luca oth Varasi, Mario oth Mercurio, Ciro oth Enthalten in Elsevier Science Jose, Ajay ELSEVIER Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles 2018 Amsterdam [u.a.] (DE-627)ELV000457477 volume:108 year:2016 day:27 month:01 pages:53-67 extent:15 https://doi.org/10.1016/j.ejmech.2015.11.010 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV SSG-OLC-PHA 42.00 Biologie: Allgemeines VZ AR 108 2016 27 0127 53-67 15 045F 610 |
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10.1016/j.ejmech.2015.11.010 doi GBVA2016008000030.pica (DE-627)ELV019300549 (ELSEVIER)S0223-5234(15)30347-0 DE-627 ger DE-627 rakwb eng 610 610 DE-600 570 540 VZ BIODIV DE-30 fid 42.00 bkl Thaler, Florian verfasserin aut Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors 2016 15 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier In the last decades, inhibitors of histone deacetylases (HDAC) have become an important class of anti-cancer agents. In a previous study we described the synthesis of spiro[chromane-2,4′-piperidine]hydroxamic acid derivatives able to inhibit histone deacetylase enzymes. Herein, we present our exploration for new derivatives by replacing the piperidine moiety with various cycloamines. The goal was to obtain highly potent compounds with a good in vitro ADME profile. In addition, molecular modeling studies unravelled the binding mode of these inhibitors. Antiproliferation Elsevier Molecular modeling Elsevier Epigenetics Elsevier Privileged structures Elsevier Histone deacetylases Elsevier Moretti, Loris oth Amici, Raffaella oth Abate, Agnese oth Colombo, Andrea oth Carenzi, Giacomo oth Fulco, Maria Carmela oth Boggio, Roberto oth Dondio, Giulio oth Gagliardi, Stefania oth Minucci, Saverio oth Sartori, Luca oth Varasi, Mario oth Mercurio, Ciro oth Enthalten in Elsevier Science Jose, Ajay ELSEVIER Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles 2018 Amsterdam [u.a.] (DE-627)ELV000457477 volume:108 year:2016 day:27 month:01 pages:53-67 extent:15 https://doi.org/10.1016/j.ejmech.2015.11.010 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV SSG-OLC-PHA 42.00 Biologie: Allgemeines VZ AR 108 2016 27 0127 53-67 15 045F 610 |
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10.1016/j.ejmech.2015.11.010 doi GBVA2016008000030.pica (DE-627)ELV019300549 (ELSEVIER)S0223-5234(15)30347-0 DE-627 ger DE-627 rakwb eng 610 610 DE-600 570 540 VZ BIODIV DE-30 fid 42.00 bkl Thaler, Florian verfasserin aut Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors 2016 15 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier In the last decades, inhibitors of histone deacetylases (HDAC) have become an important class of anti-cancer agents. In a previous study we described the synthesis of spiro[chromane-2,4′-piperidine]hydroxamic acid derivatives able to inhibit histone deacetylase enzymes. Herein, we present our exploration for new derivatives by replacing the piperidine moiety with various cycloamines. The goal was to obtain highly potent compounds with a good in vitro ADME profile. In addition, molecular modeling studies unravelled the binding mode of these inhibitors. Antiproliferation Elsevier Molecular modeling Elsevier Epigenetics Elsevier Privileged structures Elsevier Histone deacetylases Elsevier Moretti, Loris oth Amici, Raffaella oth Abate, Agnese oth Colombo, Andrea oth Carenzi, Giacomo oth Fulco, Maria Carmela oth Boggio, Roberto oth Dondio, Giulio oth Gagliardi, Stefania oth Minucci, Saverio oth Sartori, Luca oth Varasi, Mario oth Mercurio, Ciro oth Enthalten in Elsevier Science Jose, Ajay ELSEVIER Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles 2018 Amsterdam [u.a.] (DE-627)ELV000457477 volume:108 year:2016 day:27 month:01 pages:53-67 extent:15 https://doi.org/10.1016/j.ejmech.2015.11.010 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV SSG-OLC-PHA 42.00 Biologie: Allgemeines VZ AR 108 2016 27 0127 53-67 15 045F 610 |
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10.1016/j.ejmech.2015.11.010 doi GBVA2016008000030.pica (DE-627)ELV019300549 (ELSEVIER)S0223-5234(15)30347-0 DE-627 ger DE-627 rakwb eng 610 610 DE-600 570 540 VZ BIODIV DE-30 fid 42.00 bkl Thaler, Florian verfasserin aut Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors 2016 15 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier In the last decades, inhibitors of histone deacetylases (HDAC) have become an important class of anti-cancer agents. In a previous study we described the synthesis of spiro[chromane-2,4′-piperidine]hydroxamic acid derivatives able to inhibit histone deacetylase enzymes. Herein, we present our exploration for new derivatives by replacing the piperidine moiety with various cycloamines. The goal was to obtain highly potent compounds with a good in vitro ADME profile. In addition, molecular modeling studies unravelled the binding mode of these inhibitors. Antiproliferation Elsevier Molecular modeling Elsevier Epigenetics Elsevier Privileged structures Elsevier Histone deacetylases Elsevier Moretti, Loris oth Amici, Raffaella oth Abate, Agnese oth Colombo, Andrea oth Carenzi, Giacomo oth Fulco, Maria Carmela oth Boggio, Roberto oth Dondio, Giulio oth Gagliardi, Stefania oth Minucci, Saverio oth Sartori, Luca oth Varasi, Mario oth Mercurio, Ciro oth Enthalten in Elsevier Science Jose, Ajay ELSEVIER Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles 2018 Amsterdam [u.a.] (DE-627)ELV000457477 volume:108 year:2016 day:27 month:01 pages:53-67 extent:15 https://doi.org/10.1016/j.ejmech.2015.11.010 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV SSG-OLC-PHA 42.00 Biologie: Allgemeines VZ AR 108 2016 27 0127 53-67 15 045F 610 |
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10.1016/j.ejmech.2015.11.010 doi GBVA2016008000030.pica (DE-627)ELV019300549 (ELSEVIER)S0223-5234(15)30347-0 DE-627 ger DE-627 rakwb eng 610 610 DE-600 570 540 VZ BIODIV DE-30 fid 42.00 bkl Thaler, Florian verfasserin aut Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors 2016 15 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier In the last decades, inhibitors of histone deacetylases (HDAC) have become an important class of anti-cancer agents. In a previous study we described the synthesis of spiro[chromane-2,4′-piperidine]hydroxamic acid derivatives able to inhibit histone deacetylase enzymes. Herein, we present our exploration for new derivatives by replacing the piperidine moiety with various cycloamines. The goal was to obtain highly potent compounds with a good in vitro ADME profile. In addition, molecular modeling studies unravelled the binding mode of these inhibitors. Antiproliferation Elsevier Molecular modeling Elsevier Epigenetics Elsevier Privileged structures Elsevier Histone deacetylases Elsevier Moretti, Loris oth Amici, Raffaella oth Abate, Agnese oth Colombo, Andrea oth Carenzi, Giacomo oth Fulco, Maria Carmela oth Boggio, Roberto oth Dondio, Giulio oth Gagliardi, Stefania oth Minucci, Saverio oth Sartori, Luca oth Varasi, Mario oth Mercurio, Ciro oth Enthalten in Elsevier Science Jose, Ajay ELSEVIER Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles 2018 Amsterdam [u.a.] (DE-627)ELV000457477 volume:108 year:2016 day:27 month:01 pages:53-67 extent:15 https://doi.org/10.1016/j.ejmech.2015.11.010 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV SSG-OLC-PHA 42.00 Biologie: Allgemeines VZ AR 108 2016 27 0127 53-67 15 045F 610 |
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Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors |
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Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles |
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synthesis, biological characterization and molecular modeling insights of spirochromanes as potent hdac inhibitors |
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Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors |
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In the last decades, inhibitors of histone deacetylases (HDAC) have become an important class of anti-cancer agents. In a previous study we described the synthesis of spiro[chromane-2,4′-piperidine]hydroxamic acid derivatives able to inhibit histone deacetylase enzymes. Herein, we present our exploration for new derivatives by replacing the piperidine moiety with various cycloamines. The goal was to obtain highly potent compounds with a good in vitro ADME profile. In addition, molecular modeling studies unravelled the binding mode of these inhibitors. |
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In the last decades, inhibitors of histone deacetylases (HDAC) have become an important class of anti-cancer agents. In a previous study we described the synthesis of spiro[chromane-2,4′-piperidine]hydroxamic acid derivatives able to inhibit histone deacetylase enzymes. Herein, we present our exploration for new derivatives by replacing the piperidine moiety with various cycloamines. The goal was to obtain highly potent compounds with a good in vitro ADME profile. In addition, molecular modeling studies unravelled the binding mode of these inhibitors. |
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In the last decades, inhibitors of histone deacetylases (HDAC) have become an important class of anti-cancer agents. In a previous study we described the synthesis of spiro[chromane-2,4′-piperidine]hydroxamic acid derivatives able to inhibit histone deacetylase enzymes. Herein, we present our exploration for new derivatives by replacing the piperidine moiety with various cycloamines. The goal was to obtain highly potent compounds with a good in vitro ADME profile. In addition, molecular modeling studies unravelled the binding mode of these inhibitors. |
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Moretti, Loris Amici, Raffaella Abate, Agnese Colombo, Andrea Carenzi, Giacomo Fulco, Maria Carmela Boggio, Roberto Dondio, Giulio Gagliardi, Stefania Minucci, Saverio Sartori, Luca Varasi, Mario Mercurio, Ciro |
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