三氟甲基取代马蹄金素衍生物的合成及其抗乙肝病毒活性研究

Jing Cui; Wei Lu; Jing Ying Qiu; Xiao Ping Zeng; Guang Yi Liang; Bi Xue Xu

doi:10.11669/cpj.2019.13.002

三氟甲基取代马蹄金素衍生物的合成及其抗乙肝病毒活性研究

Translated title of the contribution: Synthesis and Anti-HBV Activity Evaluation of Matijin-Su Derivatives Containing Trifluoromethyl

Jing Cui, Wei Lu, Jing Ying Qiu, Xiao Ping Zeng, Guang Yi Liang^*, Bi Xue Xu

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

3 Scopus citations

Abstract

OBJECTIVE: To design and synthesize derivatives of Matijin-Su (MTS) containing trifluoromethyl group and investigate their anti-HBV activities in vitro. METHODS: Taking MTS as lead compound, target compounds were prepared by acylation, alkylation and hydrolysis, etc. The cytotoxicities and anti-HBV activities of the target compounds were tested with MTT method.RESULTS Twenty derivatives of MTS containing trifluoromethyl were synthesized and their structures were confirmed by ¹H-NMR, ¹³C-NMR and MS(ESI). The anti-HBV activities of those compounds were evaluated in HepG2 2.2.15 cells. The screening RESULTS: showed that compounds 3b, 6a, 6c, 6d, 6h-6j and 6n had HBV inhibitory effect for HepG2 2.2.15 cells. Compounds 3b, 6d and 6n exhibited significant anti-HBV activity with IC₅₀ values of 11.74, 8.73 and 11.41 μmol•L^-1. CONCLUSION: Incorporation of trifluoromethyl into MTS derivatives can lead to profound changes in their anti-HBV activity, and could be worth of further research.

Translated title of the contribution	Synthesis and Anti-HBV Activity Evaluation of Matijin-Su Derivatives Containing Trifluoromethyl
Original language	Chinese (Traditional)
Pages (from-to)	1045-1053
Number of pages	9
Journal	Chinese Pharmaceutical Journal
Volume	54
Issue number	13
DOIs	https://doi.org/10.11669/cpj.2019.13.002
State	Published - 8 Jul 2019
Externally published	Yes

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@article{6706aec5f839421d91b8fc59ac82f5b4,

title = "三氟甲基取代马蹄金素衍生物的合成及其抗乙肝病毒活性研究",

abstract = "OBJECTIVE: To design and synthesize derivatives of Matijin-Su (MTS) containing trifluoromethyl group and investigate their anti-HBV activities in vitro. METHODS: Taking MTS as lead compound, target compounds were prepared by acylation, alkylation and hydrolysis, etc. The cytotoxicities and anti-HBV activities of the target compounds were tested with MTT method.RESULTS Twenty derivatives of MTS containing trifluoromethyl were synthesized and their structures were confirmed by 1H-NMR, 13C-NMR and MS(ESI). The anti-HBV activities of those compounds were evaluated in HepG2 2.2.15 cells. The screening RESULTS: showed that compounds 3b, 6a, 6c, 6d, 6h-6j and 6n had HBV inhibitory effect for HepG2 2.2.15 cells. Compounds 3b, 6d and 6n exhibited significant anti-HBV activity with IC50 values of 11.74, 8.73 and 11.41 μmol•L-1. CONCLUSION: Incorporation of trifluoromethyl into MTS derivatives can lead to profound changes in their anti-HBV activity, and could be worth of further research.",

keywords = "Anti-hepatitis B virus activity, Matijin-Su derivatives, Synthesis, Trifluoromethyl",

author = "Jing Cui and Wei Lu and Qiu, \{Jing Ying\} and Zeng, \{Xiao Ping\} and Liang, \{Guang Yi\} and Xu, \{Bi Xue\}",

year = "2019",

month = jul,

day = "8",

doi = "10.11669/cpj.2019.13.002",

language = "繁体中文",

volume = "54",

pages = "1045--1053",

journal = "Chinese Pharmaceutical Journal",

issn = "1001-2494",

publisher = "Chinese Pharmaceutical Association",

number = "13",

}

TY - JOUR

T1 - 三氟甲基取代马蹄金素衍生物的合成及其抗乙肝病毒活性研究

AU - Cui, Jing

AU - Lu, Wei

AU - Qiu, Jing Ying

AU - Zeng, Xiao Ping

AU - Liang, Guang Yi

AU - Xu, Bi Xue

PY - 2019/7/8

Y1 - 2019/7/8

N2 - OBJECTIVE: To design and synthesize derivatives of Matijin-Su (MTS) containing trifluoromethyl group and investigate their anti-HBV activities in vitro. METHODS: Taking MTS as lead compound, target compounds were prepared by acylation, alkylation and hydrolysis, etc. The cytotoxicities and anti-HBV activities of the target compounds were tested with MTT method.RESULTS Twenty derivatives of MTS containing trifluoromethyl were synthesized and their structures were confirmed by 1H-NMR, 13C-NMR and MS(ESI). The anti-HBV activities of those compounds were evaluated in HepG2 2.2.15 cells. The screening RESULTS: showed that compounds 3b, 6a, 6c, 6d, 6h-6j and 6n had HBV inhibitory effect for HepG2 2.2.15 cells. Compounds 3b, 6d and 6n exhibited significant anti-HBV activity with IC50 values of 11.74, 8.73 and 11.41 μmol•L-1. CONCLUSION: Incorporation of trifluoromethyl into MTS derivatives can lead to profound changes in their anti-HBV activity, and could be worth of further research.

AB - OBJECTIVE: To design and synthesize derivatives of Matijin-Su (MTS) containing trifluoromethyl group and investigate their anti-HBV activities in vitro. METHODS: Taking MTS as lead compound, target compounds were prepared by acylation, alkylation and hydrolysis, etc. The cytotoxicities and anti-HBV activities of the target compounds were tested with MTT method.RESULTS Twenty derivatives of MTS containing trifluoromethyl were synthesized and their structures were confirmed by 1H-NMR, 13C-NMR and MS(ESI). The anti-HBV activities of those compounds were evaluated in HepG2 2.2.15 cells. The screening RESULTS: showed that compounds 3b, 6a, 6c, 6d, 6h-6j and 6n had HBV inhibitory effect for HepG2 2.2.15 cells. Compounds 3b, 6d and 6n exhibited significant anti-HBV activity with IC50 values of 11.74, 8.73 and 11.41 μmol•L-1. CONCLUSION: Incorporation of trifluoromethyl into MTS derivatives can lead to profound changes in their anti-HBV activity, and could be worth of further research.

KW - Anti-hepatitis B virus activity

KW - Matijin-Su derivatives

KW - Synthesis

KW - Trifluoromethyl

UR - https://www.scopus.com/pages/publications/85072680950

U2 - 10.11669/cpj.2019.13.002

DO - 10.11669/cpj.2019.13.002

M3 - 文章

AN - SCOPUS:85072680950

SN - 1001-2494

VL - 54

SP - 1045

EP - 1053

JO - Chinese Pharmaceutical Journal

JF - Chinese Pharmaceutical Journal

IS - 13

ER -

三氟甲基取代马蹄金素衍生物的合成及其抗乙肝病毒活性研究

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