Abstract
New modifications to the scaffold of previously reported HBV capsid assembly effectors such as BAY 41-4109, HAP-12 and GLS4 were explored. The anti-HBV activity in the HepAD38 system, and cytotoxicity profiles of each of the new compounds has been assessed. Among them, five new iodo- and bromo-heteroarylpyrimidines analogs displayed anti-HBV activity in the low micromolar range.
Keywords:
Capsid assembly effectors; HAP; HBV; Heteroarylpyrimidine.
Copyright © 2017 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Antiviral Agents / chemical synthesis*
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Antiviral Agents / chemistry
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Antiviral Agents / pharmacology
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Capsid Proteins / chemistry
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Capsid Proteins / metabolism*
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Cell Line
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Cell Survival / drug effects
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Chlorocebus aethiops
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Hep G2 Cells
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Hepatitis B virus / physiology*
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Humans
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Pyridines / chemistry
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry*
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Pyrimidines / pharmacology
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Structure-Activity Relationship
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Vero Cells
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Virus Replication / drug effects
Substances
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Antiviral Agents
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BAY 41-4109
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Capsid Proteins
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Pyridines
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Pyrimidines