192064-31-6Relevant academic research and scientific papers
Optimising inhibitors of trypanothione reductase using solid-phase chemistry
Chitkul, Bordin,Bradley, Mark
, p. 2367 - 2369 (2007/10/03)
A series of inhibitors of the enzyme trypanothione reductase has been identified using directed solid-phase chemistry. The compounds were based on a series of polyamine scaffolds and used the natural product kukoamine A as the lead structure. A compound with a K(i) of 76 nM was identified, although somewhat surprisingly the compound appeared to be noncompetitive in nature. (C) 2000 Elsevier Science Ltd.
Inhibition of the tissue factor/factor VIIa complex - Lead optimisation using combinatorial chemistry
Roussel, Patrick,Bradley, Mark,Kane, Peter,Bailey, Christine,Arnold, Ruth,Cross, Andrew
, p. 6219 - 6230 (2007/10/03)
Following a high throughput screen (HTS) for the inhibition of the tissue factor/factor VIIa complex and the identification of a number of original hits a lead optimisation programme was initiated to improve their potency. This necessitated the development of an amidine based linker which allowed the generation of a library of amidinonaphthols prepared both by multiple parallel synthesis (MPS) and split and mix methods. The most active compound had an IC50 of 4μM some 10x more potent than the original lead compound.
Internal resin capture - A self purification method for the synthesis of C-terminally modified peptides
Davies, Michael,Bradley, Mark
, p. 4733 - 4746 (2007/10/03)
A synthetic strategy which allows for the general modification of peptides at the C-terminus has long been the goal of the synthetic chemist. We report here the full synthetic details of our inversion and modification methodology demonstrating the method with the synthesis of peptide amides, alcohols, nitriles and a range of other modified peptides.
