3 research outputs found
Synthesis and Biological Evaluation of (<i>E</i>)ā4-Hydroxy-3-methylbut-2-enyl Phosphate (HMBP) Aryloxy Triester Phosphoramidate Prodrugs as Activators of VĪ³9/VĪ“2 TāCell Immune Responses
The aryloxy triester
phosphoramidate prodrug approach has been
used with success in drug discovery. Herein, we describe the first
application of this prodrug technology to the monophosphate derivative
of the phosphoantigen HMBPP and one of its analogues. Some of these
prodrugs exhibited specific and potent activation of VĪ³9/VĪ“2
T-cells, which were then able to lyse bladder cancer cells in vitro.
This work highlights the promise of this prodrug technology in the
discovery of novel immunotherapeutics
Synthesis and Biological Evaluation of (<i>E</i>)ā4-Hydroxy-3-methylbut-2-enyl Phosphate (HMBP) Aryloxy Triester Phosphoramidate Prodrugs as Activators of VĪ³9/VĪ“2 TāCell Immune Responses
The aryloxy triester
phosphoramidate prodrug approach has been
used with success in drug discovery. Herein, we describe the first
application of this prodrug technology to the monophosphate derivative
of the phosphoantigen HMBPP and one of its analogues. Some of these
prodrugs exhibited specific and potent activation of VĪ³9/VĪ“2
T-cells, which were then able to lyse bladder cancer cells in vitro.
This work highlights the promise of this prodrug technology in the
discovery of novel immunotherapeutics
Organometallic Nucleoside Analogues with Ferrocenyl Linker Groups: Synthesis and Cancer Cell Line Studies
Examples
of organometallic compounds as nucleoside analogues are
rare within the field of medicinal bioorganometallic chemistry. We
report on the synthesis and properties of two chiral ferrocene derivatives
containing a nucleobase and a hydroxyalkyl group. These so-called
ferronucleosides show promising anticancer activity, with cytostatic
studies on five different cancer cell lines indicating that both functional
groups are required for optimal activity