Design, synthesis, and biological evaluation of novel 7-deazapurine nucleoside derivatives as potential anti-dengue virus agents
Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pu...
Ausführliche Beschreibung
Gespeichert in:
| Autor*in: |
Lin, Cai [verfasserIn] |
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| Format: |
E-Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
2018transfer abstract |
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| Umfang: |
11 |
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| Übergeordnetes Werk: |
Enthalten in: Modeling and prediction of surface roughness for running-in wear using Gauss-Newton algorithm and ANN - Hanief, M. ELSEVIER, 2015transfer abstract, a multidisciplinary journal of antiviral agents, natural host defence mechanisms, interferons and antiviral vaccines : an official publication of the International Society for Antiviral Research, Amsterdam [u.a.] |
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| Übergeordnetes Werk: |
volume:149 ; year:2018 ; pages:95-105 ; extent:11 |
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| DOI / URN: |
10.1016/j.antiviral.2017.11.005 |
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ELV041495527 |
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| 520 | |a Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. | ||
| 520 | |a Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. | ||
| 650 | 7 | |a Dengue fever |2 Elsevier | |
| 650 | 7 | |a Nucleoside analogs |2 Elsevier | |
| 650 | 7 | |a Anti-DENV |2 Elsevier | |
| 700 | 1 | |a Yu, Jianchen |4 oth | |
| 700 | 1 | |a Hussain, Muzammal |4 oth | |
| 700 | 1 | |a Zhou, Yiqian |4 oth | |
| 700 | 1 | |a Duan, Anna |4 oth | |
| 700 | 1 | |a Pan, Weiqi |4 oth | |
| 700 | 1 | |a Yuan, Jie |4 oth | |
| 700 | 1 | |a Zhang, Jiancun |4 oth | |
| 773 | 0 | 8 | |i Enthalten in |n Elsevier Science |a Hanief, M. ELSEVIER |t Modeling and prediction of surface roughness for running-in wear using Gauss-Newton algorithm and ANN |d 2015transfer abstract |d a multidisciplinary journal of antiviral agents, natural host defence mechanisms, interferons and antiviral vaccines : an official publication of the International Society for Antiviral Research |g Amsterdam [u.a.] |w (DE-627)ELV012905879 |
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10.1016/j.antiviral.2017.11.005 doi GBV00000000000276A.pica (DE-627)ELV041495527 (ELSEVIER)S0166-3542(17)30317-0 DE-627 ger DE-627 rakwb eng 610 610 DE-600 670 VZ 530 VZ 660 VZ 000 150 VZ 54.74 bkl Lin, Cai verfasserin aut Design, synthesis, and biological evaluation of novel 7-deazapurine nucleoside derivatives as potential anti-dengue virus agents 2018transfer abstract 11 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. Dengue fever Elsevier Nucleoside analogs Elsevier Anti-DENV Elsevier Yu, Jianchen oth Hussain, Muzammal oth Zhou, Yiqian oth Duan, Anna oth Pan, Weiqi oth Yuan, Jie oth Zhang, Jiancun oth Enthalten in Elsevier Science Hanief, M. ELSEVIER Modeling and prediction of surface roughness for running-in wear using Gauss-Newton algorithm and ANN 2015transfer abstract a multidisciplinary journal of antiviral agents, natural host defence mechanisms, interferons and antiviral vaccines : an official publication of the International Society for Antiviral Research Amsterdam [u.a.] (DE-627)ELV012905879 volume:149 year:2018 pages:95-105 extent:11 https://doi.org/10.1016/j.antiviral.2017.11.005 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 54.74 Maschinelles Sehen VZ AR 149 2018 95-105 11 045F 610 |
| spelling |
10.1016/j.antiviral.2017.11.005 doi GBV00000000000276A.pica (DE-627)ELV041495527 (ELSEVIER)S0166-3542(17)30317-0 DE-627 ger DE-627 rakwb eng 610 610 DE-600 670 VZ 530 VZ 660 VZ 000 150 VZ 54.74 bkl Lin, Cai verfasserin aut Design, synthesis, and biological evaluation of novel 7-deazapurine nucleoside derivatives as potential anti-dengue virus agents 2018transfer abstract 11 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. Dengue fever Elsevier Nucleoside analogs Elsevier Anti-DENV Elsevier Yu, Jianchen oth Hussain, Muzammal oth Zhou, Yiqian oth Duan, Anna oth Pan, Weiqi oth Yuan, Jie oth Zhang, Jiancun oth Enthalten in Elsevier Science Hanief, M. ELSEVIER Modeling and prediction of surface roughness for running-in wear using Gauss-Newton algorithm and ANN 2015transfer abstract a multidisciplinary journal of antiviral agents, natural host defence mechanisms, interferons and antiviral vaccines : an official publication of the International Society for Antiviral Research Amsterdam [u.a.] (DE-627)ELV012905879 volume:149 year:2018 pages:95-105 extent:11 https://doi.org/10.1016/j.antiviral.2017.11.005 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 54.74 Maschinelles Sehen VZ AR 149 2018 95-105 11 045F 610 |
| allfields_unstemmed |
10.1016/j.antiviral.2017.11.005 doi GBV00000000000276A.pica (DE-627)ELV041495527 (ELSEVIER)S0166-3542(17)30317-0 DE-627 ger DE-627 rakwb eng 610 610 DE-600 670 VZ 530 VZ 660 VZ 000 150 VZ 54.74 bkl Lin, Cai verfasserin aut Design, synthesis, and biological evaluation of novel 7-deazapurine nucleoside derivatives as potential anti-dengue virus agents 2018transfer abstract 11 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. Dengue fever Elsevier Nucleoside analogs Elsevier Anti-DENV Elsevier Yu, Jianchen oth Hussain, Muzammal oth Zhou, Yiqian oth Duan, Anna oth Pan, Weiqi oth Yuan, Jie oth Zhang, Jiancun oth Enthalten in Elsevier Science Hanief, M. ELSEVIER Modeling and prediction of surface roughness for running-in wear using Gauss-Newton algorithm and ANN 2015transfer abstract a multidisciplinary journal of antiviral agents, natural host defence mechanisms, interferons and antiviral vaccines : an official publication of the International Society for Antiviral Research Amsterdam [u.a.] (DE-627)ELV012905879 volume:149 year:2018 pages:95-105 extent:11 https://doi.org/10.1016/j.antiviral.2017.11.005 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 54.74 Maschinelles Sehen VZ AR 149 2018 95-105 11 045F 610 |
| allfieldsGer |
10.1016/j.antiviral.2017.11.005 doi GBV00000000000276A.pica (DE-627)ELV041495527 (ELSEVIER)S0166-3542(17)30317-0 DE-627 ger DE-627 rakwb eng 610 610 DE-600 670 VZ 530 VZ 660 VZ 000 150 VZ 54.74 bkl Lin, Cai verfasserin aut Design, synthesis, and biological evaluation of novel 7-deazapurine nucleoside derivatives as potential anti-dengue virus agents 2018transfer abstract 11 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. Dengue fever Elsevier Nucleoside analogs Elsevier Anti-DENV Elsevier Yu, Jianchen oth Hussain, Muzammal oth Zhou, Yiqian oth Duan, Anna oth Pan, Weiqi oth Yuan, Jie oth Zhang, Jiancun oth Enthalten in Elsevier Science Hanief, M. ELSEVIER Modeling and prediction of surface roughness for running-in wear using Gauss-Newton algorithm and ANN 2015transfer abstract a multidisciplinary journal of antiviral agents, natural host defence mechanisms, interferons and antiviral vaccines : an official publication of the International Society for Antiviral Research Amsterdam [u.a.] (DE-627)ELV012905879 volume:149 year:2018 pages:95-105 extent:11 https://doi.org/10.1016/j.antiviral.2017.11.005 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 54.74 Maschinelles Sehen VZ AR 149 2018 95-105 11 045F 610 |
| allfieldsSound |
10.1016/j.antiviral.2017.11.005 doi GBV00000000000276A.pica (DE-627)ELV041495527 (ELSEVIER)S0166-3542(17)30317-0 DE-627 ger DE-627 rakwb eng 610 610 DE-600 670 VZ 530 VZ 660 VZ 000 150 VZ 54.74 bkl Lin, Cai verfasserin aut Design, synthesis, and biological evaluation of novel 7-deazapurine nucleoside derivatives as potential anti-dengue virus agents 2018transfer abstract 11 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. Dengue fever Elsevier Nucleoside analogs Elsevier Anti-DENV Elsevier Yu, Jianchen oth Hussain, Muzammal oth Zhou, Yiqian oth Duan, Anna oth Pan, Weiqi oth Yuan, Jie oth Zhang, Jiancun oth Enthalten in Elsevier Science Hanief, M. ELSEVIER Modeling and prediction of surface roughness for running-in wear using Gauss-Newton algorithm and ANN 2015transfer abstract a multidisciplinary journal of antiviral agents, natural host defence mechanisms, interferons and antiviral vaccines : an official publication of the International Society for Antiviral Research Amsterdam [u.a.] (DE-627)ELV012905879 volume:149 year:2018 pages:95-105 extent:11 https://doi.org/10.1016/j.antiviral.2017.11.005 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 54.74 Maschinelles Sehen VZ AR 149 2018 95-105 11 045F 610 |
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Enthalten in Modeling and prediction of surface roughness for running-in wear using Gauss-Newton algorithm and ANN Amsterdam [u.a.] volume:149 year:2018 pages:95-105 extent:11 |
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Enthalten in Modeling and prediction of surface roughness for running-in wear using Gauss-Newton algorithm and ANN Amsterdam [u.a.] volume:149 year:2018 pages:95-105 extent:11 |
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Modeling and prediction of surface roughness for running-in wear using Gauss-Newton algorithm and ANN |
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Lin, Cai @@aut@@ Yu, Jianchen @@oth@@ Hussain, Muzammal @@oth@@ Zhou, Yiqian @@oth@@ Duan, Anna @@oth@@ Pan, Weiqi @@oth@@ Yuan, Jie @@oth@@ Zhang, Jiancun @@oth@@ |
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Design, synthesis, and biological evaluation of novel 7-deazapurine nucleoside derivatives as potential anti-dengue virus agents |
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Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. |
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Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. |
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Dengue fever, caused by four distinct serotypes of dengue virus (DENV-1 to -4), has become the fastest spreading human infectious disease in recent years. Despite extensive efforts, there is no specific antiviral treatment approved for dengue until now. Nucleoside inhibitors represent an actively pursued area to develop small-molecule anti-dengue virus agents. In this study, we designed and synthesized a series of 7-deazapurine nucleoside derivatives and evaluated their anti-DENV activity. Our design strategy and structure activity relationship studies revealed 6e as the most potent inhibitor (EC50 = 2.081 ± 1.102 μM) of DENV replication. 6e suppressed RNA levels and DENV E protein expression, without causing any apparent cytotoxicity in A549 and HepG2 cells (CC50 = 150.06 ± 11.42 μM, SI = 72.11 in A549 cells, and CC50 = 146.47 ± 11.05 μM and SI = 63.7 in HepG2 cells). In addition, 6e showed similar inhibition potency against four serotypes of DENV, suggesting that it restrains some evolutionarily conserved targets essential for DENV replication. We conceive that 6e may serve as a promising lead compound for anti-DENV drug development. |
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