Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents
Identifieur interne : 000051 ( PascalFrancis/Corpus ); précédent : 000050; suivant : 000052Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents
Auteurs : Li-Jun Wang ; Chang-An Geng ; Yun-Bao Ma ; Xiao-Yan Huang ; JIE LUO ; HAO CHEN ; Rui-Hua Guo ; Xue-Mei Zhang ; Ji-Jun ChenSource :
- Bioorganic & medicinal chemistry [ 0968-0896 ] ; 2012.
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- Pascal (Inist)
English descriptors
- KwdEn :
Abstract
A series of caudatin derivatives were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the 3-0-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 21, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC50 values in the range of 2.82-7.48 μM. Interestingly, two compounds (2e, 2f) had potent activity inhibiting not only the secretion of HBsAg (IC50 = 18.68 μM, 21.71 μM), HBeAg (IC50 = 13.16 μM, 33.73 μM), but also HBV DNA replication (IC50 = 7.48 μM. 3.63 μM). The structure-activity relationships (SARs) of caudatin derivatives had been discussed, which were useful for caudatin derivatives to be explored and developed as novel anti-HBV agents.
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Format Inist (serveur)
NO : | PASCAL 12-0356332 INIST |
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ET : | Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents |
AU : | WANG (Li-Jun); GENG (Chang-An); MA (Yun-Bao); HUANG (Xiao-Yan); JIE LUO; HAO CHEN; GUO (Rui-Hua); ZHANG (Xue-Mei); CHEN (Ji-Jun) |
AF : | State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences/Kunming 650201/Chine (1 aut., 2 aut., 3 aut., 4 aut., 5 aut., 6 aut., 7 aut., 8 aut., 9 aut.); Graduate University of the Chinese Academy of Sciences/Beijing 100049/Chine (1 aut., 6 aut., 7 aut.) |
DT : | Publication en série; Niveau analytique |
SO : | Bioorganic & medicinal chemistry; ISSN 0968-0896; Pays-Bas; Da. 2012; Vol. 20; No. 9; Pp. 2877-2888 |
LA : | Anglais |
EA : | A series of caudatin derivatives were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the 3-0-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 21, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC50 values in the range of 2.82-7.48 μM. Interestingly, two compounds (2e, 2f) had potent activity inhibiting not only the secretion of HBsAg (IC50 = 18.68 μM, 21.71 μM), HBeAg (IC50 = 13.16 μM, 33.73 μM), but also HBV DNA replication (IC50 = 7.48 μM. 3.63 μM). The structure-activity relationships (SARs) of caudatin derivatives had been discussed, which were useful for caudatin derivatives to be explored and developed as novel anti-HBV agents. |
CC : | 002B02S05 |
FD : | Synthèse chimique; Relation structure activité; Activité biologique; Antiviral; Virus hépatite B; Dérivé du prégnane; Stéroïde; Caudatine dérivé |
FG : | Orthohepadnavirus; Hepadnaviridae; Virus |
ED : | Chemical synthesis; Structure activity relation; Biological activity; Antiviral; Hepatitis B virus; Pregnane derivatives; Steroid |
EG : | Orthohepadnavirus; Hepadnaviridae; Virus |
SD : | Síntesis química; Relación estructura actividad; Actividad biológica; Antiviral; Hepatitis B virus; Esteroide |
LO : | INIST-26564.354000509867520130 |
ID : | 12-0356332 |
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Pascal:12-0356332Le document en format XML
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<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Antiviral</term>
<term>Biological activity</term>
<term>Chemical synthesis</term>
<term>Hepatitis B virus</term>
<term>Pregnane derivatives</term>
<term>Steroid</term>
<term>Structure activity relation</term>
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<keywords scheme="Pascal" xml:lang="fr"><term>Synthèse chimique</term>
<term>Relation structure activité</term>
<term>Activité biologique</term>
<term>Antiviral</term>
<term>Virus hépatite B</term>
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<front><div type="abstract" xml:lang="en">A series of caudatin derivatives were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the 3-0-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 21, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC<sub>50</sub>
values in the range of 2.82-7.48 μM. Interestingly, two compounds (2e, 2f) had potent activity inhibiting not only the secretion of HBsAg (IC<sub>50</sub>
= 18.68 μM, 21.71 μM), HBeAg (IC<sub>50</sub>
= 13.16 μM, 33.73 μM), but also HBV DNA replication (IC<sub>50</sub>
= 7.48 μM. 3.63 μM). The structure-activity relationships (SARs) of caudatin derivatives had been discussed, which were useful for caudatin derivatives to be explored and developed as novel anti-HBV agents.</div>
</front>
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<fA11 i1="03" i2="1"><s1>MA (Yun-Bao)</s1>
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<fA20><s1>2877-2888</s1>
</fA20>
<fA21><s1>2012</s1>
</fA21>
<fA23 i1="01"><s0>ENG</s0>
</fA23>
<fA43 i1="01"><s1>INIST</s1>
<s2>26564</s2>
<s5>354000509867520130</s5>
</fA43>
<fA44><s0>0000</s0>
<s1>© 2012 INIST-CNRS. All rights reserved.</s1>
</fA44>
<fA47 i1="01" i2="1"><s0>12-0356332</s0>
</fA47>
<fA60><s1>P</s1>
</fA60>
<fA61><s0>A</s0>
</fA61>
<fA64 i1="01" i2="1"><s0>Bioorganic & medicinal chemistry</s0>
</fA64>
<fA66 i1="01"><s0>NLD</s0>
</fA66>
<fA99><s0>1/4 p. ref. et notes</s0>
</fA99>
<fC01 i1="01" l="ENG"><s0>A series of caudatin derivatives were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the 3-0-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 21, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC<sub>50</sub>
values in the range of 2.82-7.48 μM. Interestingly, two compounds (2e, 2f) had potent activity inhibiting not only the secretion of HBsAg (IC<sub>50</sub>
= 18.68 μM, 21.71 μM), HBeAg (IC<sub>50</sub>
= 13.16 μM, 33.73 μM), but also HBV DNA replication (IC<sub>50</sub>
= 7.48 μM. 3.63 μM). The structure-activity relationships (SARs) of caudatin derivatives had been discussed, which were useful for caudatin derivatives to be explored and developed as novel anti-HBV agents.</s0>
</fC01>
<fC02 i1="01" i2="X"><s0>002B02S05</s0>
</fC02>
<fC03 i1="01" i2="X" l="FRE"><s0>Synthèse chimique</s0>
<s5>01</s5>
</fC03>
<fC03 i1="01" i2="X" l="ENG"><s0>Chemical synthesis</s0>
<s5>01</s5>
</fC03>
<fC03 i1="01" i2="X" l="SPA"><s0>Síntesis química</s0>
<s5>01</s5>
</fC03>
<fC03 i1="02" i2="X" l="FRE"><s0>Relation structure activité</s0>
<s5>02</s5>
</fC03>
<fC03 i1="02" i2="X" l="ENG"><s0>Structure activity relation</s0>
<s5>02</s5>
</fC03>
<fC03 i1="02" i2="X" l="SPA"><s0>Relación estructura actividad</s0>
<s5>02</s5>
</fC03>
<fC03 i1="03" i2="X" l="FRE"><s0>Activité biologique</s0>
<s5>03</s5>
</fC03>
<fC03 i1="03" i2="X" l="ENG"><s0>Biological activity</s0>
<s5>03</s5>
</fC03>
<fC03 i1="03" i2="X" l="SPA"><s0>Actividad biológica</s0>
<s5>03</s5>
</fC03>
<fC03 i1="04" i2="X" l="FRE"><s0>Antiviral</s0>
<s5>04</s5>
</fC03>
<fC03 i1="04" i2="X" l="ENG"><s0>Antiviral</s0>
<s5>04</s5>
</fC03>
<fC03 i1="04" i2="X" l="SPA"><s0>Antiviral</s0>
<s5>04</s5>
</fC03>
<fC03 i1="05" i2="X" l="FRE"><s0>Virus hépatite B</s0>
<s2>NW</s2>
<s5>05</s5>
</fC03>
<fC03 i1="05" i2="X" l="ENG"><s0>Hepatitis B virus</s0>
<s2>NW</s2>
<s5>05</s5>
</fC03>
<fC03 i1="05" i2="X" l="SPA"><s0>Hepatitis B virus</s0>
<s2>NW</s2>
<s5>05</s5>
</fC03>
<fC03 i1="06" i2="X" l="FRE"><s0>Dérivé du prégnane</s0>
<s2>FR</s2>
<s5>23</s5>
</fC03>
<fC03 i1="06" i2="X" l="ENG"><s0>Pregnane derivatives</s0>
<s2>FR</s2>
<s5>23</s5>
</fC03>
<fC03 i1="07" i2="X" l="FRE"><s0>Stéroïde</s0>
<s5>24</s5>
</fC03>
<fC03 i1="07" i2="X" l="ENG"><s0>Steroid</s0>
<s5>24</s5>
</fC03>
<fC03 i1="07" i2="X" l="SPA"><s0>Esteroide</s0>
<s5>24</s5>
</fC03>
<fC03 i1="08" i2="X" l="FRE"><s0>Caudatine dérivé</s0>
<s4>INC</s4>
<s5>86</s5>
</fC03>
<fC07 i1="01" i2="X" l="FRE"><s0>Orthohepadnavirus</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="01" i2="X" l="ENG"><s0>Orthohepadnavirus</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="01" i2="X" l="SPA"><s0>Orthohepadnavirus</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="02" i2="X" l="FRE"><s0>Hepadnaviridae</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="02" i2="X" l="ENG"><s0>Hepadnaviridae</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="02" i2="X" l="SPA"><s0>Hepadnaviridae</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="03" i2="X" l="FRE"><s0>Virus</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="03" i2="X" l="ENG"><s0>Virus</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="03" i2="X" l="SPA"><s0>Virus</s0>
<s2>NW</s2>
</fC07>
<fN21><s1>275</s1>
</fN21>
<fN44 i1="01"><s1>OTO</s1>
</fN44>
<fN82><s1>OTO</s1>
</fN82>
</pA>
</standard>
<server><NO>PASCAL 12-0356332 INIST</NO>
<ET>Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents</ET>
<AU>WANG (Li-Jun); GENG (Chang-An); MA (Yun-Bao); HUANG (Xiao-Yan); JIE LUO; HAO CHEN; GUO (Rui-Hua); ZHANG (Xue-Mei); CHEN (Ji-Jun)</AU>
<AF>State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences/Kunming 650201/Chine (1 aut., 2 aut., 3 aut., 4 aut., 5 aut., 6 aut., 7 aut., 8 aut., 9 aut.); Graduate University of the Chinese Academy of Sciences/Beijing 100049/Chine (1 aut., 6 aut., 7 aut.)</AF>
<DT>Publication en série; Niveau analytique</DT>
<SO>Bioorganic & medicinal chemistry; ISSN 0968-0896; Pays-Bas; Da. 2012; Vol. 20; No. 9; Pp. 2877-2888</SO>
<LA>Anglais</LA>
<EA>A series of caudatin derivatives were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the 3-0-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 21, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC<sub>50</sub>
values in the range of 2.82-7.48 μM. Interestingly, two compounds (2e, 2f) had potent activity inhibiting not only the secretion of HBsAg (IC<sub>50</sub>
= 18.68 μM, 21.71 μM), HBeAg (IC<sub>50</sub>
= 13.16 μM, 33.73 μM), but also HBV DNA replication (IC<sub>50</sub>
= 7.48 μM. 3.63 μM). The structure-activity relationships (SARs) of caudatin derivatives had been discussed, which were useful for caudatin derivatives to be explored and developed as novel anti-HBV agents.</EA>
<CC>002B02S05</CC>
<FD>Synthèse chimique; Relation structure activité; Activité biologique; Antiviral; Virus hépatite B; Dérivé du prégnane; Stéroïde; Caudatine dérivé</FD>
<FG>Orthohepadnavirus; Hepadnaviridae; Virus</FG>
<ED>Chemical synthesis; Structure activity relation; Biological activity; Antiviral; Hepatitis B virus; Pregnane derivatives; Steroid</ED>
<EG>Orthohepadnavirus; Hepadnaviridae; Virus</EG>
<SD>Síntesis química; Relación estructura actividad; Actividad biológica; Antiviral; Hepatitis B virus; Esteroide</SD>
<LO>INIST-26564.354000509867520130</LO>
<ID>12-0356332</ID>
</server>
</inist>
</record>
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