CycloSal-2'-ara(ribo)-fluoro-2',3'-dideoxyadenosine monophosphates--an effort to solve the structure-activity relationship of 2'-fluoro-ddA

C Meier; T Knispel; V E Marquez; E De Clercq; J Balzarini

doi:10.1080/15257779908041598

CycloSal-2'-ara(ribo)-fluoro-2',3'-dideoxyadenosine monophosphates--an effort to solve the structure-activity relationship of 2'-fluoro-ddA

Nucleosides Nucleotides. 1999 Apr-May;18(4-5):907-12. doi: 10.1080/15257779908041598.

Authors

C Meier¹, T Knispel, V E Marquez, E De Clercq, J Balzarini

Affiliation

¹ Institut für Organische Chemie, Universität Hamburg, Germany.

PMID: 10432708
DOI: 10.1080/15257779908041598

Abstract

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.

MeSH terms

Dideoxyadenosine / analogs & derivatives*
Dideoxyadenosine / chemistry
Dideoxyadenosine / pharmacology
Reverse Transcriptase Inhibitors / chemistry
Reverse Transcriptase Inhibitors / pharmacology
Structure-Activity Relationship

Substances

Reverse Transcriptase Inhibitors
Dideoxyadenosine