Gallium and indium complexes with new hexadentate bis(semicarbazone) and bis(thiosemicarbazone) chelators

Author(s): Viviana S. Prado ¹ ^, ² ^, ³ ^, ⁴ , Renan C. F. Leitao ¹ ^, ² ^, ³ ^, ⁴ , Francisco Silva ⁵ ^, ⁶ ^, ⁷ ^, ⁸ ^, ⁹ , Lurdes Gano ⁵ ^, ⁶ ^, ⁷ ^, ⁸ ^, ⁹ , Isabel C. Santos ⁵ ^, ⁶ ^, ⁷ ^, ⁸ ^, ⁹ , Fabio L. N. Marques ¹⁰ ^, ¹¹ ^, ¹² ^, ¹³ ^, ¹⁴ , António Paulo ⁵ ^, ⁶ ^, ⁷ ^, ⁸ ^, ⁹ , Victor M. Deflon ¹ ^, ² ^, ³ ^, ⁴

Publication date (Electronic): 2021

Journal: Dalton Transactions

Publisher: Royal Society of Chemistry (RSC)

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Abstract

Rapid, low temperature and high yield synthesis of ⁶⁷Ga and ¹¹¹In radiocomplexes with new hexadentate bis(semicarbazone) and bis(thiosemicarbazone) chelators.

Abstract

The synthesis of two new hexadentate potentially tetra-anionic acyclic chelators, an N ₂O ₄-donor bis(semicarbazone) ( H4bsc) and an N ₂O ₂S ₂-donor bis(thiosemicarbazone) ( H4btsc), is described. Coordination reactions of the ligands with gallium and indium precursors were investigated and yielded the complexes [Ga(Hbsc)] ( 1) and [In(Hbtsc)] ( 2), respectively. Ligands and complexes structures were confirmed by several techniques, including FTIR, NMR ( ¹H, ¹³C, COSY, HSQC), ESI(+)-MS and single crystal X-ray diffraction analysis. The radioactive congeners [ ⁶⁷Ga(Hbsc)] ( 1*) and [ ¹¹¹In(Hbtsc)] ( 2*) were also synthesized and their radiolabeling yield and radiochemical purity were certified by HPLC and ITLC analyses. Biodistribution assays in groups of CD-1 mice showed a high uptake of both radiocomplexes in liver and intestine where 1* presented higher retention. In vitro and in vivo assays revealed higher stability of 1* compared with 2*, namely in the blood. The results suggest that radiocomplex 1* is a candidate for further investigation as it could be prepared in high yields (>95%), at low temperature (20–25 °C) and at fast reaction time (15 min), which are very desirable synthesis conditions for potential new radiopharmaceuticals.

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A short history of SHELX

George M. Sheldrick (2008)

An account is given of the development of the SHELX system of computer programs from SHELX -76 to the present day. In addition to identifying useful innovations that have come into general use through their implementation in SHELX , a critical analysis is presented of the less-successful features, missed opportunities and desirable improvements for future releases of the software. An attempt is made to understand how a program originally designed for photographic intensity data, punched cards and computers over 10000 times slower than an average modern personal computer has managed to survive for so long. SHELXL is the most widely used program for small-molecule refinement and SHELXS and SHELXD are often employed for structure solution despite the availability of objectively superior programs. SHELXL also finds a niche for the refinement of macromolecules against high-resolution or twinned data; SHELXPRO acts as an interface for macromolecular applications. SHELXC , SHELXD and SHELXE are proving useful for the experimental phasing of macromolecules, especially because they are fast and robust and so are often employed in pipelines for high-throughput phasing. This paper could serve as a general literature citation when one or more of the open-source SHELX programs (and the Bruker AXS version SHELXTL ) are employed in the course of a crystal-structure determination.