title: Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
abstract: A novel series of CXCR4 antagonists were identified based on the substantial redesign of AMD070. These compounds possessed potent anti-HIV-1 activity and showed excellent pharmacokinetics in rat and dog.
authors.affiliation: Genzyme Corp., Waltham, MA 02451, USA. renato.skerlj@genzyme.com
authors.forename: Renato
authors.initials: R
authors.lastname: Skerlj
authors.forename: Gary
authors.initials: G
authors.lastname: Bridger
authors.forename: Ernest
authors.initials: E
authors.lastname: McEachern
authors.forename: Curtis
authors.initials: C
authors.lastname: Harwig
authors.forename: Chris
authors.initials: C
authors.lastname: Smith
authors.forename: Alan
authors.initials: A
authors.lastname: Kaller
authors.forename: Duane
authors.initials: D
authors.lastname: Veale
authors.forename: Helen
authors.initials: H
authors.lastname: Yee
authors.forename: Krystyna
authors.initials: K
authors.lastname: Skupinska
authors.forename: Rossana
authors.initials: R
authors.lastname: Wauthy
authors.forename: Letian
authors.initials: L
authors.lastname: Wang
authors.forename: Ian
authors.initials: I
authors.lastname: Baird
authors.forename: Yongbao
authors.initials: Y
authors.lastname: Zhu
authors.forename: Kate
authors.initials: K
authors.lastname: Burrage
authors.forename: Wen
authors.initials: W
authors.lastname: Yang
authors.forename: Michael
authors.initials: M
authors.lastname: Sartori
authors.forename: Dana
authors.initials: D
authors.lastname: Huskens
authors.forename: Erik
authors.initials: E
authors.lastname: De Clercq
authors.forename: Dominique
authors.initials: D
authors.lastname: Schols
mesh_terms: D000634:Aminoquinolines; D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D001562:Benzimidazoles; D002082:Butylamines; D004261:DNA Replication / Q000187:drug effects; D004285:Dogs; D015195:Drug Design; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry; D015394:Molecular Structure; D051381:Rats; D019718:Receptors, CXCR4 / Q000037:antagonists & inhibitors*; D014779:Virus Replication / Q000187:drug effects*
chemical_list: D000634:Aminoquinolines; D019380:Anti-HIV Agents; D001562:Benzimidazoles; D002082:Butylamines; D006573:Heterocyclic Compounds, 1-Ring; D019718:Receptors, CXCR4; C494414:mavorixafor