title: Synthesis and antiviral evaluation of novel heteroarylpyrimidines analogs as HBV capsid effectors.
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.
authors.affiliation: Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
authors.forename: Sebastien
authors.initials: S
authors.lastname: Boucle
authors.affiliation: Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
authors.forename: Xiao
authors.initials: X
authors.lastname: Lu
authors.affiliation: Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
authors.forename: Leda
authors.initials: L
authors.lastname: Bassit
authors.affiliation: Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
authors.forename: Tugba
authors.initials: T
authors.lastname: Ozturk
authors.affiliation: Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
authors.forename: Olivia Ollinger
authors.initials: OO
authors.lastname: Russell
authors.affiliation: Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
authors.forename: Franck
authors.initials: F
authors.lastname: Amblard
authors.affiliation: Cocrystal Pharma, Inc., 1860 Montreal Road, Tucker, GA 30084, USA.
authors.forename: Steven J
authors.initials: SJ
authors.lastname: Coats
authors.affiliation: Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA. Electronic address: rschina@emory.edu.
authors.forename: Raymond F
authors.initials: RF
authors.lastname: Schinazi
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D036022:Capsid Proteins / Q000737:chemistry / Q000378:metabolism*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D056945:Hep G2 Cells; D006515:Hepatitis B virus / Q000502:physiology*; D006801:Humans; D011725:Pyridines / Q000737:chemistry; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014709:Vero Cells; D014779:Virus Replication / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; C464059:BAY 41-4109; D036022:Capsid Proteins; D011725:Pyridines; D011743:Pyrimidines
keywords: Capsid assembly effectors; HAP; HBV; Heteroarylpyrimidine