Scientists crack code for tracking experimental cancer drugs in the body
Researchers have solved a long-standing chemistry problem that blocks the ability to monitor how experimental cancer medicines move through patients during clinical trials. The breakthrough could accelerate testing of promising treatments and help doctors personalize drug dosing for better outcomes.
Originaltitel: <sup>18</sup>F-labelling of nitrogen-containing aryl boronates: anti-cancer drug melflufen as a case study
<p><sup>18</sup>F-labelling of nitrogen-containing arenes <em>via</em> copper-mediated radiofluorination (CMRF) was investigated. The studies targeted the analogues of the anti-cancer drug melflufen with an alkylating bis(2-chloroethyl)amino pharmacophore. Studies of the melflufen analogues and various model compounds indicated that the copper mediated boron–fluorine-18 exchange reaction is affected differently by the three nitrogen-containing groups in the target compound. The largest inhibitory effects on the fluorine labelling process were exerted by the tertiary amine based bis(2-chloroethyl)amino pharmacophore. The best results were achieved by applying bipyridyl ligands for the copper mediator.</p>