66997-19-1Relevant academic research and scientific papers
Gliotoxin analogues as inhibitors of reverse transcriptase. 1. Effect of lipophilicity.
Ottenheijm,H.C.J. et al.
, p. 796 - 799 (2007/10/08)
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.
