title: Design and synthesis of novel threosyl-5'- deoxyphosphonic acid purine analogues as potent anti-HIV agents.
abstract: The discovery of threosyl phosphonate nucleoside (PMDTA, EC₅₀ = 2.53 μM) as a potent anti-HIV agent has led to the synthesis and biological evaluation of 5 '-deoxyversions of threosyl phosphonate nucleosides from 1,4-dihydroxy-2-butene. The synthesized nucleoside phosphonic acid analogues 14 and 19 were tested for anti-HIV activity as well as cytotoxicity. The adenine analogue 14 exhibits moderate in vitro anti-HIV-1 activity (EC₅₀ = 12.6 μM).
authors.affiliation: BK-21 Project Team, College of Pharmacy, Chosun University, Kwangju, Republic of Korea.
authors.forename: Lian Jin
authors.initials: LJ
authors.lastname: Liu
authors.forename: Eunae
authors.initials: E
authors.lastname: Kim
authors.forename: Joon Hee
authors.initials: JH
authors.lastname: Hong
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002522:Chlorocebus aethiops; D015195:Drug Design; D015497:HIV-1 / Q000187:drug effects*; D063065:Organophosphonates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D011687:Purines / Q000737:chemistry*; D014709:Vero Cells
chemical_list: D019380:Anti-HIV Agents; D063065:Organophosphonates; D011687:Purines