Synthesis and anti-HIV activities of phorbol derivatives
In this study, 37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated, building upon our previous synthesis of 51 phorbol derivatives. 12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out, demonstrating remarkable anti-HIV-1 activit...
Ausführliche Beschreibung
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| Autor*in: |
HUANG, Xiaolei [verfasserIn] TANG, Chengrun [verfasserIn] HUANG, Xusheng [verfasserIn] YANG, Yun [verfasserIn] LI, Qirun [verfasserIn] MA, Mengdi [verfasserIn] ZHAO, Lei [verfasserIn] YANG, Liumeng [verfasserIn] CUI, Yadong [verfasserIn] ZHANG, Zhenqing [verfasserIn] ZHENG, Yongtang [verfasserIn] ZHANG, Jian [verfasserIn] |
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| Format: |
E-Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
2024 |
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| Schlagwörter: |
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| Übergeordnetes Werk: |
Enthalten in: No title available - 22, Seite 146-160 |
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| Übergeordnetes Werk: |
volume:22 ; pages:146-160 |
| DOI / URN: |
10.1016/S1875-5364(24)60587-X |
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ELV066998247 |
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| 520 | |a In this study, 37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated, building upon our previous synthesis of 51 phorbol derivatives. 12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out, demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia formation. These derivatives exhibited a higher safety index compared with the positive control drug. Among them, 12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol, designated as compound 3c, exhibited the most potent anti-HIV-1 activity (EC50 2.9 nmol·L−1, CC50/EC50 11 117.24) and significantly inhibited the formation of syncytium (EC50 7.0 nmol·L−1, CC50/EC50 4891.43). Moreover, compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase inhibitor. Isothermal titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C (PKC). Therefore, compound 3c emerges as a potential candidate for developing new anti-HIV drugs. | ||
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| 650 | 4 | |a Anti-HIV-1 activity | |
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10.1016/S1875-5364(24)60587-X doi (DE-627)ELV066998247 (ELSEVIER)S1875-5364(24)60587-X DE-627 ger DE-627 rda eng HUANG, Xiaolei verfasserin aut Synthesis and anti-HIV activities of phorbol derivatives 2024 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In this study, 37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated, building upon our previous synthesis of 51 phorbol derivatives. 12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out, demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia formation. These derivatives exhibited a higher safety index compared with the positive control drug. Among them, 12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol, designated as compound 3c, exhibited the most potent anti-HIV-1 activity (EC50 2.9 nmol·L−1, CC50/EC50 11 117.24) and significantly inhibited the formation of syncytium (EC50 7.0 nmol·L−1, CC50/EC50 4891.43). Moreover, compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase inhibitor. Isothermal titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C (PKC). Therefore, compound 3c emerges as a potential candidate for developing new anti-HIV drugs. Phorbol esters Anti-HIV-1 activity Syncytia formation 12-( Safety index HIV-1 entry inhibitor HIV-1 reverse transcriptase inhibitor PKC activator TANG, Chengrun verfasserin aut HUANG, Xusheng verfasserin aut YANG, Yun verfasserin aut LI, Qirun verfasserin aut MA, Mengdi verfasserin aut ZHAO, Lei verfasserin aut YANG, Liumeng verfasserin aut CUI, Yadong verfasserin aut ZHANG, Zhenqing verfasserin aut ZHENG, Yongtang verfasserin aut ZHANG, Jian verfasserin aut Enthalten in No title available 22, Seite 146-160 (DE-627)574362789 1875-5364 nnns volume:22 pages:146-160 GBV_USEFLAG_U GBV_ELV SYSFLAG_U GBV_ILN_2004 GBV_ILN_2015 AR 22 146-160 |
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10.1016/S1875-5364(24)60587-X doi (DE-627)ELV066998247 (ELSEVIER)S1875-5364(24)60587-X DE-627 ger DE-627 rda eng HUANG, Xiaolei verfasserin aut Synthesis and anti-HIV activities of phorbol derivatives 2024 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In this study, 37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated, building upon our previous synthesis of 51 phorbol derivatives. 12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out, demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia formation. These derivatives exhibited a higher safety index compared with the positive control drug. Among them, 12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol, designated as compound 3c, exhibited the most potent anti-HIV-1 activity (EC50 2.9 nmol·L−1, CC50/EC50 11 117.24) and significantly inhibited the formation of syncytium (EC50 7.0 nmol·L−1, CC50/EC50 4891.43). Moreover, compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase inhibitor. Isothermal titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C (PKC). Therefore, compound 3c emerges as a potential candidate for developing new anti-HIV drugs. Phorbol esters Anti-HIV-1 activity Syncytia formation 12-( Safety index HIV-1 entry inhibitor HIV-1 reverse transcriptase inhibitor PKC activator TANG, Chengrun verfasserin aut HUANG, Xusheng verfasserin aut YANG, Yun verfasserin aut LI, Qirun verfasserin aut MA, Mengdi verfasserin aut ZHAO, Lei verfasserin aut YANG, Liumeng verfasserin aut CUI, Yadong verfasserin aut ZHANG, Zhenqing verfasserin aut ZHENG, Yongtang verfasserin aut ZHANG, Jian verfasserin aut Enthalten in No title available 22, Seite 146-160 (DE-627)574362789 1875-5364 nnns volume:22 pages:146-160 GBV_USEFLAG_U GBV_ELV SYSFLAG_U GBV_ILN_2004 GBV_ILN_2015 AR 22 146-160 |
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10.1016/S1875-5364(24)60587-X doi (DE-627)ELV066998247 (ELSEVIER)S1875-5364(24)60587-X DE-627 ger DE-627 rda eng HUANG, Xiaolei verfasserin aut Synthesis and anti-HIV activities of phorbol derivatives 2024 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In this study, 37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated, building upon our previous synthesis of 51 phorbol derivatives. 12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out, demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia formation. These derivatives exhibited a higher safety index compared with the positive control drug. Among them, 12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol, designated as compound 3c, exhibited the most potent anti-HIV-1 activity (EC50 2.9 nmol·L−1, CC50/EC50 11 117.24) and significantly inhibited the formation of syncytium (EC50 7.0 nmol·L−1, CC50/EC50 4891.43). Moreover, compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase inhibitor. Isothermal titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C (PKC). Therefore, compound 3c emerges as a potential candidate for developing new anti-HIV drugs. Phorbol esters Anti-HIV-1 activity Syncytia formation 12-( Safety index HIV-1 entry inhibitor HIV-1 reverse transcriptase inhibitor PKC activator TANG, Chengrun verfasserin aut HUANG, Xusheng verfasserin aut YANG, Yun verfasserin aut LI, Qirun verfasserin aut MA, Mengdi verfasserin aut ZHAO, Lei verfasserin aut YANG, Liumeng verfasserin aut CUI, Yadong verfasserin aut ZHANG, Zhenqing verfasserin aut ZHENG, Yongtang verfasserin aut ZHANG, Jian verfasserin aut Enthalten in No title available 22, Seite 146-160 (DE-627)574362789 1875-5364 nnns volume:22 pages:146-160 GBV_USEFLAG_U GBV_ELV SYSFLAG_U GBV_ILN_2004 GBV_ILN_2015 AR 22 146-160 |
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10.1016/S1875-5364(24)60587-X doi (DE-627)ELV066998247 (ELSEVIER)S1875-5364(24)60587-X DE-627 ger DE-627 rda eng HUANG, Xiaolei verfasserin aut Synthesis and anti-HIV activities of phorbol derivatives 2024 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In this study, 37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated, building upon our previous synthesis of 51 phorbol derivatives. 12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out, demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia formation. These derivatives exhibited a higher safety index compared with the positive control drug. Among them, 12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol, designated as compound 3c, exhibited the most potent anti-HIV-1 activity (EC50 2.9 nmol·L−1, CC50/EC50 11 117.24) and significantly inhibited the formation of syncytium (EC50 7.0 nmol·L−1, CC50/EC50 4891.43). Moreover, compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase inhibitor. Isothermal titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C (PKC). Therefore, compound 3c emerges as a potential candidate for developing new anti-HIV drugs. Phorbol esters Anti-HIV-1 activity Syncytia formation 12-( Safety index HIV-1 entry inhibitor HIV-1 reverse transcriptase inhibitor PKC activator TANG, Chengrun verfasserin aut HUANG, Xusheng verfasserin aut YANG, Yun verfasserin aut LI, Qirun verfasserin aut MA, Mengdi verfasserin aut ZHAO, Lei verfasserin aut YANG, Liumeng verfasserin aut CUI, Yadong verfasserin aut ZHANG, Zhenqing verfasserin aut ZHENG, Yongtang verfasserin aut ZHANG, Jian verfasserin aut Enthalten in No title available 22, Seite 146-160 (DE-627)574362789 1875-5364 nnns volume:22 pages:146-160 GBV_USEFLAG_U GBV_ELV SYSFLAG_U GBV_ILN_2004 GBV_ILN_2015 AR 22 146-160 |
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10.1016/S1875-5364(24)60587-X doi (DE-627)ELV066998247 (ELSEVIER)S1875-5364(24)60587-X DE-627 ger DE-627 rda eng HUANG, Xiaolei verfasserin aut Synthesis and anti-HIV activities of phorbol derivatives 2024 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In this study, 37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated, building upon our previous synthesis of 51 phorbol derivatives. 12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out, demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia formation. These derivatives exhibited a higher safety index compared with the positive control drug. Among them, 12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol, designated as compound 3c, exhibited the most potent anti-HIV-1 activity (EC50 2.9 nmol·L−1, CC50/EC50 11 117.24) and significantly inhibited the formation of syncytium (EC50 7.0 nmol·L−1, CC50/EC50 4891.43). Moreover, compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase inhibitor. Isothermal titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C (PKC). Therefore, compound 3c emerges as a potential candidate for developing new anti-HIV drugs. Phorbol esters Anti-HIV-1 activity Syncytia formation 12-( Safety index HIV-1 entry inhibitor HIV-1 reverse transcriptase inhibitor PKC activator TANG, Chengrun verfasserin aut HUANG, Xusheng verfasserin aut YANG, Yun verfasserin aut LI, Qirun verfasserin aut MA, Mengdi verfasserin aut ZHAO, Lei verfasserin aut YANG, Liumeng verfasserin aut CUI, Yadong verfasserin aut ZHANG, Zhenqing verfasserin aut ZHENG, Yongtang verfasserin aut ZHANG, Jian verfasserin aut Enthalten in No title available 22, Seite 146-160 (DE-627)574362789 1875-5364 nnns volume:22 pages:146-160 GBV_USEFLAG_U GBV_ELV SYSFLAG_U GBV_ILN_2004 GBV_ILN_2015 AR 22 146-160 |
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HUANG, Xiaolei TANG, Chengrun HUANG, Xusheng YANG, Yun LI, Qirun MA, Mengdi ZHAO, Lei YANG, Liumeng CUI, Yadong ZHANG, Zhenqing ZHENG, Yongtang ZHANG, Jian |
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Elektronische Aufsätze |
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HUANG, Xiaolei |
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10.1016/S1875-5364(24)60587-X |
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verfasserin |
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synthesis and anti-hiv activities of phorbol derivatives |
| title_auth |
Synthesis and anti-HIV activities of phorbol derivatives |
| abstract |
In this study, 37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated, building upon our previous synthesis of 51 phorbol derivatives. 12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out, demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia formation. These derivatives exhibited a higher safety index compared with the positive control drug. Among them, 12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol, designated as compound 3c, exhibited the most potent anti-HIV-1 activity (EC50 2.9 nmol·L−1, CC50/EC50 11 117.24) and significantly inhibited the formation of syncytium (EC50 7.0 nmol·L−1, CC50/EC50 4891.43). Moreover, compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase inhibitor. Isothermal titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C (PKC). Therefore, compound 3c emerges as a potential candidate for developing new anti-HIV drugs. |
| abstractGer |
In this study, 37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated, building upon our previous synthesis of 51 phorbol derivatives. 12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out, demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia formation. These derivatives exhibited a higher safety index compared with the positive control drug. Among them, 12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol, designated as compound 3c, exhibited the most potent anti-HIV-1 activity (EC50 2.9 nmol·L−1, CC50/EC50 11 117.24) and significantly inhibited the formation of syncytium (EC50 7.0 nmol·L−1, CC50/EC50 4891.43). Moreover, compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase inhibitor. Isothermal titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C (PKC). Therefore, compound 3c emerges as a potential candidate for developing new anti-HIV drugs. |
| abstract_unstemmed |
In this study, 37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated, building upon our previous synthesis of 51 phorbol derivatives. 12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out, demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia formation. These derivatives exhibited a higher safety index compared with the positive control drug. Among them, 12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol, designated as compound 3c, exhibited the most potent anti-HIV-1 activity (EC50 2.9 nmol·L−1, CC50/EC50 11 117.24) and significantly inhibited the formation of syncytium (EC50 7.0 nmol·L−1, CC50/EC50 4891.43). Moreover, compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase inhibitor. Isothermal titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C (PKC). Therefore, compound 3c emerges as a potential candidate for developing new anti-HIV drugs. |
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GBV_USEFLAG_U GBV_ELV SYSFLAG_U GBV_ILN_2004 GBV_ILN_2015 |
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Synthesis and anti-HIV activities of phorbol derivatives |
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TANG, Chengrun HUANG, Xusheng YANG, Yun LI, Qirun MA, Mengdi ZHAO, Lei YANG, Liumeng CUI, Yadong ZHANG, Zhenqing ZHENG, Yongtang ZHANG, Jian |
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TANG, Chengrun HUANG, Xusheng YANG, Yun LI, Qirun MA, Mengdi ZHAO, Lei YANG, Liumeng CUI, Yadong ZHANG, Zhenqing ZHENG, Yongtang ZHANG, Jian |
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2024-07-06T19:44:05.078Z |
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