An alternative synthesis of Vandetanib (CaprelsaTM) via a microwave accelerated Dimroth rearrangement

YesVandetanib is an orally available tyrosine kinase inhibitor used in the treatment of cancer. The current synthesis proceeds via an unstable 4-chloroquinazoline, using harsh reagents, in addition to requiring sequential protection and deprotection steps. In the present work, use of the Dimroth rearrangement in the key quinazoline forming step enabled the synthesis of Vandetanib in nine steps (compared to the previously reported 12–14).This work was supported by the Cancer Research UK-Cancer Imaging Centre (grant: C1060/ A16464), the Institute of Cancer Research and the University of Hull

Smart bandages – A colourful approach to early stage infection detection & control in wound care

With the recent increase in bacterial resistance to conventional antibiotics, the early-stage detection and control of infection has become imperative in the fight against opportunistic pathogens in healthcare. The traditional β-lactam wonder-drugs (e.g. penicillin and cephalosporins), are rendered inactive due to enzymatic hydrolysis by bacterial β-lactamase enzymes as a bacterial defence mechanism. However, this deactivation mechanism produces different responses in the two aforementioned drugs - with the cephalosporins showing a molecular rearrangement mechanism which could be utilised for prodrug delivery. This unique mechanism could mean that inactive forms of cephalosporin antibiotics, once used as chemotherapeutics in oncology, could once again be used in the fight against disease as sensors to detect and treat bacterial colonisation. Therefore, we hypothesize that cephalosporin-dye bandages might provide an effective method to visually detect, and subsequently control, the early stages of an infection using photoantimicrobial chemotherapy (PACT)