Targeting of epigenetic mechanisms, such as the hydroxymethylation of DNA, has been intensively studied, with respect to the treatment of many serious pathologies, including oncological disorders. Recent studies demonstrated that promising therapeutic strategies could potentially be based on the inhibition of the TET1 protein (ten-eleven translocation methylcytosine dioxygenase 1) by specific iron chelators. Therefore, in the present work, we prepared a series of pyrrolopyrrole derivatives with hydrazide (1) or hydrazone (2–6) iron-binding groups. As a result, we determined that the basic pyrrolo[3,2-b]pyrrole derivative 1 was a strong inhibitor of the TET1 protein (IC50 = 1.33 μM), supported by microscale thermophoresis and molecular docking. Pyrrolo[3,2-b]pyrroles 2–6, bearing substituted 2-hydroxybenzylidene moieties, displayed no significant inhibitory activity. In addition, in vitro studies demonstrated that derivative 1 exhibits potent anticancer activity and an exclusive mitochondrial localization, confirmed by Pearson’s correlation coefficient of 0.92.
Hydrofluoroethers (HFEs) represent a new family of promising engineering fluids suitable for technical cleaning and cooling of electronic and magnetic devices or as admixtures in refrigerant blends. Here, we report accurate data for the liquid density at 0.1 MPa and temperatures from $$273.15\,\text{K}$$ 273.15 K to $$343.15\,\text{K}$$ 343.15 K for a series of five HFEs, namely, HFE-7000, HFE-7100, HFE-7200, HFE-7300, and HFE-7500. A highly sensitive vibrating tube densimeter with a borosilicate glass U-tube calibrated according to the procedure by Prokopová et al. (J Chem Thermodyn 173:106855, 2022) provided density data with an expanded uncertainty ($$k=2$$ k = 2 ) of $$0.13\,\text{kg}\cdot \text{m}^{-3}$$ 0.13 kg · m - 3 . Influences such as sample degassing, water content, or sample temperature before its dosing into the densimeter are discussed. Thanks to the high sensitivity of the used densimeter, an unexpected shift in the density of different HFE-7100 and HFE-7200 liquid samples was detected. Unlike other HFEs, HFE-7100 and HFE-7200 are mixtures of two hardly separable isomers, which were so far considered having identical thermophysical properties. Utilizing nuclear magnetic resonance spectroscopy, the ratio of n-isomer and iso-isomer was inspected for various liquid samples. In the range of iso-isomer mole fraction from 0.61 to 0.77, the new measurements revealed density differences of more than $$5\,\text{kg}\cdot \text{m}^{-3}$$ 5 kg · m - 3 in case of HFE-7100 and of about $$3\,\text{kg}\cdot \text{m}^{-3}$$ 3 kg · m - 3 in case of HFE-7200. Consequently, for some applications, the properties of different HFE isomers cannot be considered identical. The Rackett-type correlation for the saturated liquid density was fitted using the new and the literature data.
Hydrofluoroethers (HFEs) represent a new family of promising engineering fluids suitable for technical cleaning, cooling of electronic and magnetic devices or as admixtures in refrigerant blends. Here we report accurate data for the liquid density at 0.1\,MPa and temperatures from $273.15\,\mathrm{K}$ to $343.15\,\mathrm{K}$ for a series of five HFEs; namely HFE-7000, HFE-7100, HFE-7200, HFE-7300, and HFE-7500. A highly sensitive vibrating tube densimeter with a borosilicate glass U-tube calibrated according to the procedure by Prokopov\'{a} et al. [J. Chem. Thermodyn. 173 (2022) 106855] provided density data with an expanded uncertainty ($k=2$) of $0.13\,\mathrm{kg\cdot m^{-3}}$. Influences such as sample degassing, water content or sample temperature before its dosing into the densimeter are discussed. Thanks to the high sensitivity of the used densimeter, an unexpected shift in the density of different HFE-7100 and HFE-7200 liquid samples was detected. Unlike other HFEs, HFE-7100 and HFE-7200 are mixtures of two hardly separable isomers, which were so far considered having identical thermophysical properties. Utilizing nuclear magnetic resonance spectroscopy, the ratio of \textit{n}-isomer and \textit{iso}-isomer was inspected for various liquid samples. In the range of \textit{iso}-isomer mole fraction from 0.61 to 0.77, the new measurements revealed density differences of more than $5\,\mathrm{kg\cdot m^{-3}}$ in case of HFE-7100 and of about $3\,\mathrm{kg\cdot m^{-3}}$ in case of HFE-7200. Consequently, for some applications the properties of different HFE isomers cannot be considered identical. The Rackett-type correlation for the saturated liquid density was fitted using the new and the literature data.
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