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Four new palladium complexes containing a cyclometallated pinane ligand and l-amino acids (proline, tyrosine, serine, isoleucine) as coligands were synthesized and characterized. For the synthesis, we used the previously described binuclear palladacycle, the opening of the chloride bridges in which provides easy introduction of additional biogenic ligands and obtaining multimodal palladium complexes. All newly obtained compounds were characterized by NMR and IR spectroscopy and elemental analysis. We studied the antitumor activity of the synthesized complexes and reference compounds expressed in their toxic effect against a panel of tumor-derived cell lines A549, SH-SY5Y, Hep-2, and HeLa. It was established that the cytotoxic effect of the palladacycles may be due to the ability of these compounds to cause destruction of mitochondria by depolarizing the mitochondrial membrane. Some structure—activity correlations were revealed. [ABSTRACT FROM AUTHOR]

Six new chiral zinc(ii) complexes 1–6 based on ethylenediamine derivatives of terpenes were synthesized and characterized. The molecular structure of complex 2 was established by X-ray diffraction analysis. The modulating effect of complexes 1–6 on the functional state of mitochondria, which are organelles playing an utterly important role in maintaining the energy balance of cells, transfer of genetic material, and regulation of the processes of triggering the cell death by apoptosis, autophagy, and necrosis, was studied. It is shown that synthesized zinc complexes lead to depolarization of the mitochondrial membrane, an increase in the threshold of sensitivity of the organelles to calcium-induced opening of the mitochondrial permeability transition pores, and disruption of the operation of the respiratory chain complexes in these organelles. Such a dysfunctional state of mitochondria is one of the main causes of cell death through apoptosis due to the release of various proapoptotic factors into the intracellular space. In this regard, the newly synthesized zinc complexes 1–6 can be considered as destructive agents aimed at triggering cell death cascades by affecting mitochondrial functions. These properties are of paramount importance when searching for potential drugs with possible antitumor, antiprotozoal, or antifungal activity. [ABSTRACT FROM AUTHOR]

Previously unknown conjugates of the natural sesquiterpene lactone arteannuin B, which was isolated from Artemisia annua, were synthesized via Michael reactions with pharmacophoric amines and tested in vitro for cytotoxic activity. The compounds were shown to exhibit antiproliferative properties for various tumor cell lines. The most active derivatives had IC50 values of 8–36 μM, which exceeded that of starting arteannuin B. Practically all obtained conjugates were found to modulate glycolysis in MCF7 tumor cells. The lead compound was the conjugate with 3-ethoxycarbonylpiperidine, which could be considered a platform for developing antitumor drugs. [ABSTRACT FROM AUTHOR]