Expertise

Medicinal Chemistry

We have extensive expertise in the design, synthesis, and biological evaluation of small molecules as therapeutics for several human diseases.  Our key expertise is in all the phases of translational developemnt of medicines from laboratory to clinic. Three anticancer agents synthesised in Cardiff are currently evaluated in human clinical trials by Nucana plc.

In addition we have extensive experience in diverse branches of organic synthesis:

Phosphoro- and Phosphonoamidate Prodrugs synthesis.

Our group is specialized in the synthesis of phosphoramidate prodrugs via phosphorus (V) and P (III) chemistries. One of the major area of expertise is in the stereoselective synthesis of these prodrugs. We have developed the first catalytic methodology to synthesise a diastereomeric enriched mixture (SP, the usually most biologically active diastereoisomer) of ProTide of anticancer and antiviral nucleosides.

diastereoselective protide

F. Pertusati and C. McGuigan; Chem. Commun., 2015, 51, 8070-8073.

Carbohydrate chemistry

Synthesis and modification of sugar-phosphate prodrugs. Our early work on glucosamine is a key example:

glucosamine

Serpi M1, Bibbo R, Rat S, et al., J. Med Chem. 2012, 55(10), 4629-39; J. Med. Chem.  51185807-5812

Fluorine Chemistry.

Part of our research is focused in using fluorinated structural motifs in the design of novel molecules with pharmacological activities or improving the properties of blockbuster drugs.

BIC                            enzal

M. Bassetto S. Ferla, F. Pertusati., Eur. J. Med. Chem. 118 (2016) 230-243;