Title: Gliotoxin analogues as inhibitors of reverse transcriptase. 1. Effect of lipophilicity
Authors: Ottenheijm, H C ×
Herscheid, J D
Tijhuis, M W
Oosterbaan, M
De Clercq, Erik #
Issue Date: Aug-1978
Publisher: ACS Publications
Series Title: Journal of Medicinal Chemistry vol:21 issue:8 pages:796-9
Abstract: The reaction scheme, developed for the synthesis of the gliotoxin analogue 2, was found to be of general applicability for analogues with varying substituents at N(1) and C(2). Analogues 11b-g prepared by this method are inhibitors of reverse transcriptase (RNA-directed DNA polymerase). Their inhibitory activity seems to be related to the lipophilicity of the effector molecules: the most lipophilic compound is the most active inhibitor. The techniques of reversed-phase thin-layer chromatography with silylated, precoated plates as well as reversed-phase high-performance liquid chromatography were used to measure the relative lipophilicities; both techniques gave analogous results.
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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