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

^*Corresponding author for this work

School of Chemistry and Molecular Engineering

East China Normal University
CAS - Shanghai Institute of Materia Medica

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

45 Scopus citations

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.

Original language	English
Pages (from-to)	5048-5055
Number of pages	8
Journal	Bioorganic and Medicinal Chemistry
Volume	18
Issue number	14
DOIs	https://doi.org/10.1016/j.bmc.2010.05.076
State	Published - 15 Jul 2010

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Anti-HBV activity
Benzimidazoles

Access to Document

10.1016/j.bmc.2010.05.076

Cite this

@article{c57f037f18924e34b55714d317173f1e,

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",

month = jul,

day = "15",

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

language = "英语",

volume = "18",

pages = "5048--5055",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

publisher = "Elsevier Ltd",

number = "14",

}

TY - JOUR

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

Abstract

UN SDGs

Keywords

Access to Document

Other files and links

Fingerprint

Cite this