Designing model imino bifunctional chelators for radiopharmaceuticals –in vitroantitumor activity, photoluminescence and structural analysis

Abstract

Designed bifunctional chelators for the radionuclides of 188/186Re or 99mTc. Structure, DFT calculations, antitumor and imaging properties are described.

Substitution reactivity and structural variability induced by tryptamine on the biomimetic rhenium tricarbonyl complex

“…Previously ((1), in the form of powder) has been investigated and demonstrated to have a quantum yield of 1.3% and 0.9% at 390 nm and 280 nm. 31 Reproducibility of the quantum yield of (1) in both forms (powder vs. crystalline) has been conrmed. The morphology of a luminescent material may have a strong effect on its emission intensity, e.g.…”

“…UV-Vis (nm, L mol À1 cm À1 ): l max ¼ 397, 3 ¼ 7.686 Â 10 2 . 31 6). ReAA (0.0500 g, 6.489 Â 10 À2 mmol) was dissolved in methanol (5 ml).…”

“…Schiff base ligands shows signicant luminescent activity without metal centres present, however depending on the metal used the Schiff base complex could exhibit variation in luminosity. [31][32][33] While in certain cases the luminescent properties of Schiff base ligands improve upon complexation with metals, particularly that from the lanthanide series, the cytotoxicity is not necessarily so predictable in either the ligand or metal complex of that ligand and therefore needs to be systematically evaluated. It should be noted that rhenium complexes with little to no chemotoxic activity can still be of great interest for the clinical practitioner if a radioisotope is used, for example 188 Re, should the complex be intended for therapy, exploiting the high energy b particles of the decaying nuclei, i.e.…”

Crystal structure and Hirshfeld surface analysis of 2-{[(E)-(3-cyclobutyl-1H-1,2,4-triazol-5-yl)imino]methyl}phenol

“…However, several related compounds have been reported that include (E)-N-benzylidene-1H-1,2,4-triazol-5-amine as the main skeleton, viz. 5-methyl-2-[(1H-1,2,4-triazol-3-ylimino)methyl]phenol (PEVXAS; Brink et al, 2018) Symmetry codes: (i) x À 2; y; z; (ii) x À 1; y; z.…”

The crystal structure of (E)-1-(quinolin-2-ylmethyl)-2-((1-(quinolin-2-ylmethyl)pyridin-2(1H)-ylidene)amino)pyridin-1-ium, C30H25BrN5

“…Pyridyl based type of ligands have contributed a great deal across many fields [9][10][11][12]. Subsequently, a great deal of interest towards multi-dentate pyridyl based ligands has grown over the decades across many disciplines including photoluminescence [13], medicinal chemistry [14], catalysis [15,16] and radiopharmaceutical [17] chemistry, also as pursued in our research group [18][19][20]. It is for this evidence that the tailoring of the multi-dentate ligands are still of paramount importance.…”