Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors
Abstract A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies le...
Ausführliche Beschreibung
Gespeichert in:
| Autor*in: |
Stammers, Timothy A. [verfasserIn] |
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| Format: |
E-Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
2013 |
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| Schlagwörter: |
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| Umfang: |
5 |
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| Übergeordnetes Werk: |
Enthalten in: Feeding European sea bass ( - Torrecillas, S. ELSEVIER, 2018, a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines, Amsterdam [u.a.] |
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| Übergeordnetes Werk: |
volume:23 ; year:2013 ; number:9 ; day:1 ; month:05 ; pages:2585-2589 ; extent:5 |
| Links: |
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| DOI / URN: |
10.1016/j.bmcl.2013.02.110 |
|---|
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ELV011760540 |
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| 520 | |a Abstract A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a–c and 12a–c from a weak-binding fragment-like structure 1 as a starting point. | ||
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10.1016/j.bmcl.2013.02.110 doi GBVA2013016000014.pica (DE-627)ELV011760540 (ELSEVIER)S0960-894X(13)00297-7 DE-627 ger DE-627 rakwb eng 540 610 540 DE-600 610 DE-600 630 VZ 22 ssgn 46.00 bkl Stammers, Timothy A. verfasserin aut Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors 2013 5 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a–c and 12a–c from a weak-binding fragment-like structure 1 as a starting point. Non-nucleoside inhibitor Elsevier Parallel synthesis Elsevier Antiviral Elsevier NS5B polymerase Elsevier Hepatitis C virus Elsevier Structure based drug design Elsevier Coulombe, René oth Rancourt, Jean oth Thavonekham, Bounkham oth Fazal, Gulrez oth Goulet, Sylvie oth Jakalian, Araz oth Wernic, Dominic oth Tsantrizos, Youla oth Poupart, Marc-André oth Bös, Michael oth McKercher, Ginette oth Thauvette, Louise oth Kukolj, George oth Beaulieu, Pierre L. oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:23 year:2013 number:9 day:1 month:05 pages:2585-2589 extent:5 https://doi.org/10.1016/j.bmcl.2013.02.110 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 23 2013 9 1 0501 2585-2589 5 045F 540 |
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10.1016/j.bmcl.2013.02.110 doi GBVA2013016000014.pica (DE-627)ELV011760540 (ELSEVIER)S0960-894X(13)00297-7 DE-627 ger DE-627 rakwb eng 540 610 540 DE-600 610 DE-600 630 VZ 22 ssgn 46.00 bkl Stammers, Timothy A. verfasserin aut Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors 2013 5 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a–c and 12a–c from a weak-binding fragment-like structure 1 as a starting point. Non-nucleoside inhibitor Elsevier Parallel synthesis Elsevier Antiviral Elsevier NS5B polymerase Elsevier Hepatitis C virus Elsevier Structure based drug design Elsevier Coulombe, René oth Rancourt, Jean oth Thavonekham, Bounkham oth Fazal, Gulrez oth Goulet, Sylvie oth Jakalian, Araz oth Wernic, Dominic oth Tsantrizos, Youla oth Poupart, Marc-André oth Bös, Michael oth McKercher, Ginette oth Thauvette, Louise oth Kukolj, George oth Beaulieu, Pierre L. oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:23 year:2013 number:9 day:1 month:05 pages:2585-2589 extent:5 https://doi.org/10.1016/j.bmcl.2013.02.110 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 23 2013 9 1 0501 2585-2589 5 045F 540 |
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10.1016/j.bmcl.2013.02.110 doi GBVA2013016000014.pica (DE-627)ELV011760540 (ELSEVIER)S0960-894X(13)00297-7 DE-627 ger DE-627 rakwb eng 540 610 540 DE-600 610 DE-600 630 VZ 22 ssgn 46.00 bkl Stammers, Timothy A. verfasserin aut Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors 2013 5 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a–c and 12a–c from a weak-binding fragment-like structure 1 as a starting point. Non-nucleoside inhibitor Elsevier Parallel synthesis Elsevier Antiviral Elsevier NS5B polymerase Elsevier Hepatitis C virus Elsevier Structure based drug design Elsevier Coulombe, René oth Rancourt, Jean oth Thavonekham, Bounkham oth Fazal, Gulrez oth Goulet, Sylvie oth Jakalian, Araz oth Wernic, Dominic oth Tsantrizos, Youla oth Poupart, Marc-André oth Bös, Michael oth McKercher, Ginette oth Thauvette, Louise oth Kukolj, George oth Beaulieu, Pierre L. oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:23 year:2013 number:9 day:1 month:05 pages:2585-2589 extent:5 https://doi.org/10.1016/j.bmcl.2013.02.110 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 23 2013 9 1 0501 2585-2589 5 045F 540 |
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10.1016/j.bmcl.2013.02.110 doi GBVA2013016000014.pica (DE-627)ELV011760540 (ELSEVIER)S0960-894X(13)00297-7 DE-627 ger DE-627 rakwb eng 540 610 540 DE-600 610 DE-600 630 VZ 22 ssgn 46.00 bkl Stammers, Timothy A. verfasserin aut Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors 2013 5 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a–c and 12a–c from a weak-binding fragment-like structure 1 as a starting point. Non-nucleoside inhibitor Elsevier Parallel synthesis Elsevier Antiviral Elsevier NS5B polymerase Elsevier Hepatitis C virus Elsevier Structure based drug design Elsevier Coulombe, René oth Rancourt, Jean oth Thavonekham, Bounkham oth Fazal, Gulrez oth Goulet, Sylvie oth Jakalian, Araz oth Wernic, Dominic oth Tsantrizos, Youla oth Poupart, Marc-André oth Bös, Michael oth McKercher, Ginette oth Thauvette, Louise oth Kukolj, George oth Beaulieu, Pierre L. oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:23 year:2013 number:9 day:1 month:05 pages:2585-2589 extent:5 https://doi.org/10.1016/j.bmcl.2013.02.110 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 23 2013 9 1 0501 2585-2589 5 045F 540 |
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10.1016/j.bmcl.2013.02.110 doi GBVA2013016000014.pica (DE-627)ELV011760540 (ELSEVIER)S0960-894X(13)00297-7 DE-627 ger DE-627 rakwb eng 540 610 540 DE-600 610 DE-600 630 VZ 22 ssgn 46.00 bkl Stammers, Timothy A. verfasserin aut Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors 2013 5 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a–c and 12a–c from a weak-binding fragment-like structure 1 as a starting point. Non-nucleoside inhibitor Elsevier Parallel synthesis Elsevier Antiviral Elsevier NS5B polymerase Elsevier Hepatitis C virus Elsevier Structure based drug design Elsevier Coulombe, René oth Rancourt, Jean oth Thavonekham, Bounkham oth Fazal, Gulrez oth Goulet, Sylvie oth Jakalian, Araz oth Wernic, Dominic oth Tsantrizos, Youla oth Poupart, Marc-André oth Bös, Michael oth McKercher, Ginette oth Thauvette, Louise oth Kukolj, George oth Beaulieu, Pierre L. oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:23 year:2013 number:9 day:1 month:05 pages:2585-2589 extent:5 https://doi.org/10.1016/j.bmcl.2013.02.110 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 23 2013 9 1 0501 2585-2589 5 045F 540 |
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Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors |
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Abstract A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a–c and 12a–c from a weak-binding fragment-like structure 1 as a starting point. |
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Abstract A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a–c and 12a–c from a weak-binding fragment-like structure 1 as a starting point. |
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Abstract A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a–c and 12a–c from a weak-binding fragment-like structure 1 as a starting point. |
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