Identification of 1-isopropylsulfonyl-2-amine benzimidazoles as a new class of inhibitors of hepatitis B virus

Yun Fei Li; Gui Feng Wang; Yu Luo; Wei Gang Huang; Wei Tang; Chun Lan Feng; Li Ping Shi; Yu Dan Ren; Jian Ping Zuo; Wei Lu

doi:10.1016/j.ejmech.2007.03.005

Identification of 1-isopropylsulfonyl-2-amine benzimidazoles as a new class of inhibitors of hepatitis B virus

Yun Fei Li
, Gui Feng Wang
, Yu Luo
, Wei Gang Huang
, Wei Tang
, Chun Lan Feng
, Li Ping Shi
, Yu Dan Ren
, Jian Ping Zuo^*
, Wei Lu

^*此作品的通讯作者

化学与分子工程学院

CAS - Shanghai Institute of Materia Medica
East China Normal University

科研成果: 期刊稿件 › 文章 › 同行评审

50 引用（Scopus）

摘要

A series of 1-isopropylsulfonyl-2-amine benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. In general, these derivatives are potent HBV inhibitors (IC₅₀ < 4 μM) with high selectivity indices (SIs > 40). Compounds 5b-e, g, j, and 9a were among the most prominent compounds, with IC₅₀s of 0.70-2.0 μM and SIs of 41-274. The potent anti-HBV activity and safety profiles of the most promising compounds 5d and j (IC₅₀s = 0.70 μM, SIs > 120) demonstrate the potential of this series of benzimidazoles for the development of new anti-HBV drugs.

源语言	英语
页（从-至）	1358-1364
页数	7
期刊	European Journal of Medicinal Chemistry
卷	42
期	11-12
DOI	https://doi.org/10.1016/j.ejmech.2007.03.005
出版状态	已出版 - 11月 2007

联合国可持续发展目标

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可持续发展目标 3 良好健康与福祉

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10.1016/j.ejmech.2007.03.005

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title = "Identification of 1-isopropylsulfonyl-2-amine benzimidazoles as a new class of inhibitors of hepatitis B virus",

abstract = "A series of 1-isopropylsulfonyl-2-amine benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. In general, these derivatives are potent HBV inhibitors (IC50 < 4 μM) with high selectivity indices (SIs > 40). Compounds 5b-e, g, j, and 9a were among the most prominent compounds, with IC50s of 0.70-2.0 μM and SIs of 41-274. The potent anti-HBV activity and safety profiles of the most promising compounds 5d and j (IC50s = 0.70 μM, SIs > 120) demonstrate the potential of this series of benzimidazoles for the development of new anti-HBV drugs.",

keywords = "Anti-HBV activity, Benzimidazoles, Synthesis",

author = "Li, \{Yun Fei\} and Wang, \{Gui Feng\} and Yu Luo and Huang, \{Wei Gang\} and Wei Tang and Feng, \{Chun Lan\} and Shi, \{Li Ping\} and Ren, \{Yu Dan\} and Zuo, \{Jian Ping\} and Wei Lu",

year = "2007",

month = nov,

doi = "10.1016/j.ejmech.2007.03.005",

language = "英语",

volume = "42",

pages = "1358--1364",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

number = "11-12",

}

TY - JOUR

T1 - Identification of 1-isopropylsulfonyl-2-amine benzimidazoles as a new class of inhibitors of hepatitis B virus

AU - Li, Yun Fei

AU - Wang, Gui Feng

AU - Luo, Yu

AU - Huang, Wei Gang

AU - Tang, Wei

AU - Feng, Chun Lan

AU - Shi, Li Ping

AU - Ren, Yu Dan

AU - Zuo, Jian Ping

AU - Lu, Wei

PY - 2007/11

Y1 - 2007/11

N2 - A series of 1-isopropylsulfonyl-2-amine benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. In general, these derivatives are potent HBV inhibitors (IC50 < 4 μM) with high selectivity indices (SIs > 40). Compounds 5b-e, g, j, and 9a were among the most prominent compounds, with IC50s of 0.70-2.0 μM and SIs of 41-274. The potent anti-HBV activity and safety profiles of the most promising compounds 5d and j (IC50s = 0.70 μM, SIs > 120) demonstrate the potential of this series of benzimidazoles for the development of new anti-HBV drugs.

AB - A series of 1-isopropylsulfonyl-2-amine benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. In general, these derivatives are potent HBV inhibitors (IC50 < 4 μM) with high selectivity indices (SIs > 40). Compounds 5b-e, g, j, and 9a were among the most prominent compounds, with IC50s of 0.70-2.0 μM and SIs of 41-274. The potent anti-HBV activity and safety profiles of the most promising compounds 5d and j (IC50s = 0.70 μM, SIs > 120) demonstrate the potential of this series of benzimidazoles for the development of new anti-HBV drugs.

KW - Anti-HBV activity

KW - Benzimidazoles

KW - Synthesis

UR - https://www.scopus.com/pages/publications/36248956157

U2 - 10.1016/j.ejmech.2007.03.005

DO - 10.1016/j.ejmech.2007.03.005

M3 - 文章

C2 - 17499889

AN - SCOPUS:36248956157

SN - 0223-5234

VL - 42

SP - 1358

EP - 1364

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 11-12

ER -

Identification of 1-isopropylsulfonyl-2-amine benzimidazoles as a new class of inhibitors of hepatitis B virus

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