The synthesis of emetine analogue NSC-134754, a potent inhibitor of the HIF pathway, has been accomplished and its structure reassigned. The stereochemistry of NSC-134754 has been assigned for the first time using X-ray crystallography and it has been demonstrated that only one diastereoisomer is active against HIF.

Facile and quantitative dissociation of bis(thiosemicarbazonato)zinc (lI) complexes to give the corresponding neutral proligands in solution has been achieved by reaction with citric acid. This reaction provides an elegant solution to a problem encountered in the design, synthesis and purification of potential copper-based radiopharmaceuticals.

The cover picture shows the structure of a pyrene‐functionalised bis(thiosemicarbazonato)copper complex that has been designed as a first‐generation dual‐modality agent for combination with in vivo positron emission tomography and in vitro fluorescence microscopy. Details of the synthesis as well as characterisation of the electronic properties by using spectroelectrochemistry, fluorescence emission spectroscopy and density functional calculations are reported in the article by J. P. Holland, J. M. Peach et al. on p. 48 ff.

The syntheses of pyrene‐functionalised bis(thiosemicarbazonato)zinc and ‐copper complexes are reported. In contrast to previously reported bis(thiosemicarbazonato)Cu2+ complexes which are nonfluorescent, the pyrene group remains highly fluorescent. The compounds have been characterised by using a wide range of techniques including reverse‐phase HPLC, cyclic voltammetry, NMR, electronic absorption (UV/Vis), infrared and fluorescence emission spectroscopy. Spectroelectrochemistry experiments demonstrated that the Cu2+ complexes undergo quasi‐reversible one‐electron reduction at biologically accessible potentials. Density functional theory calculations were used to probe the electronic structure of the pyrene‐functionalised copper complexes and confirmed that the ligand‐based fluorescent emission occurs due to the absence of orbital interactions between the pyrene and bis(thiosemicarbazonato)copper groups. These preliminary studies demonstrate that the new copper complexes have potential to be used as dual‐modality agents for in vitro cellular fluorescence microscopy and in vivo positron emission tomography experiments.

The Synthesis and Structure Revision of NSC-134754. -For the first time the X-ray structure of the target compound is determined and reassigned to (I). Only the shown diastereomer is showing the ability to inhibit HIF activity. -(HICKIN, J. A.; AHMED, A.; FUCKE, K.; ASHCROFT, M.; JONES*, K.; Chem. Commun. (Cambridge) 50 (2014) 10, 1238-1240, http://dx.