title: Uncharged AZT and D4T derivatives of phosphonoformic and phosphonoacetic acids as anti-HIV pronucleosides.
abstract: Two series of new lipophilic phosphonoformate and phosphonoacetate derivatives of AZT and d4T were synthesized and evaluated as anti-HIV agents. The efficacy of some of the synthesized compounds in cell cultures infected with HIV-1 was higher than that of the parent nucleosides and only slightly correlated to their stability in the phosphate buffer and human blood serum. The synthesized phosphonates are most probably prodrug forms of the corresponding nucleosides.
authors.affiliation: Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, 32 Vavilov str., Moscow 119991, Russian Federation. shirokova-elena@list.ru
authors.forename: Elena A
authors.initials: EA
authors.lastname: Shirokova
authors.forename: Maxim V
authors.initials: MV
authors.lastname: Jasko
authors.forename: Anastasiya L
authors.initials: AL
authors.lastname: Khandazhinskaya
authors.forename: Alexander V
authors.initials: AV
authors.lastname: Ivanov
authors.forename: Dmitry V
authors.initials: DV
authors.lastname: Yanvarev
authors.forename: Yury S
authors.initials: YS
authors.lastname: Skoblov
authors.forename: Vladimir A
authors.initials: VA
authors.lastname: Mitkevich
authors.forename: Eduard V
authors.initials: EV
authors.lastname: Bocharov
authors.forename: Tatyana R
authors.initials: TR
authors.lastname: Pronyaeva
authors.forename: Nina V
authors.initials: NV
authors.lastname: Fedyuk
authors.forename: Marina K
authors.initials: MK
authors.lastname: Kukhanova
authors.forename: Andrey G
authors.initials: AG
authors.lastname: Pokrovsky
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D004355:Drug Stability; D017245:Foscarnet / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D006868:Hydrolysis; D010746:Phosphonoacetic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D011355:Prodrugs / Q000138:chemical synthesis* / Q000494:pharmacology; D018119:Stavudine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D015215:Zidovudine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D019380:Anti-HIV Agents; D011355:Prodrugs; D017245:Foscarnet; D015215:Zidovudine; D018119:Stavudine; D010746:Phosphonoacetic Acid