Novel series of [ddN]-[TSAO-T] heterodimers as potential bi-functional inhibitors of HIV-1 RT. Studies in the linker and ddN region.
Novel series of [ddN]-(CH2)n-[TSAO-T] heterodimers have been prepared and tested for their anti-HIV-1 and HIV-2 activity. The most active compound of this series was the [d4T]-(CH2)3-[TSAO-T] heterodimer (EC50 = 0.018 +/- 0.03 microM).
Velázquez
S
S
Instituto de Química Médica (C.S.I.C.), Madrid, Spain.
Tuñón
V
V
Jimeno
M L
ML
Pérez-Pérez
M J
MJ
San-Félix
A
A
Chamorro
C
C
Lobatón
E
E
Esteban-Gamboa
A
A
De Clercq
E
E
Balzarini
J
J
Camarasa
M J
MJ
D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D019281:Dimerization; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013141:Spiro Compounds / Q000737:chemistry* / Q000494:pharmacology*; D013936:Thymidine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D014529:Uridine / Q000031:analogs & derivatives
D019380:Anti-HIV Agents; D018894:Reverse Transcriptase Inhibitors; D013141:Spiro Compounds; D054303:HIV Reverse Transcriptase; D013936:Thymidine; C075132:TSAO-T; D014529:Uridine