Tetrazines as Traceless Carriers for Polar Drugs

A recent invention in Bradford has identified a new carrier molecule that reduces the polarity of polar drugs. The modification makes significant (0.5-1 log fold) improvements to the logP of highly-polar hydroxyl compounds and is predicted to confer favourable uptake and distribution properties on any linked drug compound. The “prodrugs” undergo hydrolysis to release the parent compound.

The programme of work will provide a rounded Medicinal Chemistry education. Work will be phased so that simpler compounds are prepared and tested in the first year and a comprehensive range of chemical and biological techniques learnt. More complex targets will be attempted as the student’s experience and confidence grow.

Aim 1: Synthesis
Aim 2: Kinetics of tetrazine breakdown and drug release
Aim 3: (a) Time-dependent In Vitro Chemosensitivity; (b) Tumour Penetration Assay