Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus

Yu Luo; Jia Ping Yao; Li Yang; Chun Lan Feng; Wei Tang; Gui Feng Wang; Jian Pin Zuo; Wei Lu

doi:10.1016/j.bmc.2010.05.076

Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus

Yu Luo
, Jia Ping Yao
, Li Yang
, Chun Lan Feng
, Wei Tang
, Gui Feng Wang
, Jian Pin Zuo^*
, Wei Lu

^*此作品的通讯作者

化学与分子工程学院

East China Normal University
CAS - Shanghai Institute of Materia Medica

科研成果: 期刊稿件 › 文章 › 同行评审

45 引用（Scopus）

摘要

A series of novel benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compound 12a, with IC ₅₀ <0.41 μM and SI >81.2, was the most promising compound and selected as the benchmark compound for further optimization.

源语言	英语
页（从-至）	5048-5055
页数	8
期刊	Bioorganic and Medicinal Chemistry
卷	18
期	14
DOI	https://doi.org/10.1016/j.bmc.2010.05.076
出版状态	已出版 - 15 7月 2010

联合国可持续发展目标

此成果有助于实现下列可持续发展目标：

可持续发展目标 3 良好健康与福祉

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10.1016/j.bmc.2010.05.076

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title = "Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus",

abstract = "A series of novel benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compound 12a, with IC 50 <0.41 μM and SI >81.2, was the most promising compound and selected as the benchmark compound for further optimization.",

keywords = "Anti-HBV activity, Benzimidazoles",

author = "Yu Luo and Yao, \{Jia Ping\} and Li Yang and Feng, \{Chun Lan\} and Wei Tang and Wang, \{Gui Feng\} and Zuo, \{Jian Pin\} and Wei Lu",

year = "2010",

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doi = "10.1016/j.bmc.2010.05.076",

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T1 - Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus

AU - Luo, Yu

AU - Yao, Jia Ping

AU - Yang, Li

AU - Feng, Chun Lan

AU - Tang, Wei

AU - Wang, Gui Feng

AU - Zuo, Jian Pin

AU - Lu, Wei

PY - 2010/7/15

Y1 - 2010/7/15

N2 - A series of novel benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compound 12a, with IC 50 <0.41 μM and SI >81.2, was the most promising compound and selected as the benchmark compound for further optimization.

AB - A series of novel benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compound 12a, with IC 50 <0.41 μM and SI >81.2, was the most promising compound and selected as the benchmark compound for further optimization.

KW - Anti-HBV activity

KW - Benzimidazoles

UR - https://www.scopus.com/pages/publications/77955337993

U2 - 10.1016/j.bmc.2010.05.076

DO - 10.1016/j.bmc.2010.05.076

M3 - 文章

C2 - 20639110

AN - SCOPUS:77955337993

SN - 0968-0896

VL - 18

SP - 5048

EP - 5055

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 14

ER -

Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus

摘要

联合国可持续发展目标

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