CycloSal-2'-ara(ribo)-fluoro-2',3'-dideoxyadenosine monophosphates--an effort to solve the structure-activity relationship of 2'-fluoro-ddA.
Novel lipophilic cycloSal-triesters 3 and 4 from the ara- and ribo-configurated 2'-fluorinated ddAs 1 and 2, respectively, were prepared. The title compounds 3 and 4 delivered the corresponding monophosphates and thus, increasing the bioactivity or convert a formerly inactive compound into a RT inhibitor.
Meier
C
C
Institut für Organische Chemie, Universität Hamburg, Germany.
Knispel
T
T
Marquez
V E
VE
De Clercq
E
E
Balzarini
J
J
D016048:Dideoxyadenosine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D018894:Reverse Transcriptase Inhibitors; D016048:Dideoxyadenosine