Ternary copper(<scp>ii</scp>) complexes of 1,10-phenanthroline and coumarin-based oxylacetates as pro-apoptotic UPR CHOP inducers

Masuri, Sebastiano; Cabiddu, Maria Grazia; Moráň, Lukáš; Vesselá, Tereza; Bartosik, Martin; Havel, Josef; Meloni, Francesca; Cadoni, Enzo; Vaňhara, Petr; Pivetta, Tiziana

doi:10.1039/d3nj01317k

New J. Chem.

2023

DOI: 10.1039/d3nj01317k

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Ternary copper(ii) complexes of 1,10-phenanthroline and coumarin-based oxylacetates as pro-apoptotic UPR CHOP inducers

Sebastiano Masuri,

Maria Grazia Cabiddu,

Lukáš Moráň

et al.

Abstract: We prepared six complexes with formula [Cu(phen)2(Lx)](ClO4)(x: 1 – 6) where the auxiliary ligands Lx are coumarin carboxylate derivatives bearing an oxylacetate moiety in the 6th or 7th position and...

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2024

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Design, Synthesis, Structural Insights, Tyrosinase Inhibition, and Sun Protection Factor of New Thiosemicarbazone Derivatives

Masuri,

Era,

Pintus

et al. 2024

Molecules

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Tyrosinase, a key protein in the biosynthesis of melanin pigments, is crucial in determining skin pigmentation. Inhibiting tyrosinase activity is a promising approach for treating conditions related to excessive pigmentation. For the synthesis of more potent tyrosinase inhibitors, we combined two approaches, para-substitution and lipophilicity, to enhance the inhibitory properties of (E)-2-(4-hydroxybenzylidene)hydrazine-1-carbotiamide, whose enzyme inhibitory properties have been previously demonstrated. The newly synthesized compounds showed potent inhibition activity against tyrosinase in the micromolar concentration range. The synthesised compounds were up to 41 times more effective than kojic acid. In addition to this biological activity, all molecules were evaluated for their sun protection factor to determine their photoprotective effects. All the compounds showed higher efficacy than reference compounds, used as sunscreens in photoprotective preparations. All compounds were noncytotoxic at the concentration required to inhibit tyrosinase activity. With the aim of defining the potential binding modes and the kind of interactions between the studied molecules and the catalytic site of mushroom tyrosinase, molecular docking simulations were also performed.

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Design, Synthesis, Structural Insights, Tyrosinase Inhibition, and Sun Protection Factor of New Thiosemicarbazone Derivatives

Masuri,

Era,

Pintus

et al. 2024

Molecules

View full text Add to dashboard Cite

show abstract

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Ternary copper(ii) complexes of 1,10-phenanthroline and coumarin-based oxylacetates as pro-apoptotic UPR CHOP inducers

Abstract: We prepared six complexes with formula [Cu(phen)2(Lx)](ClO4)(x: 1 – 6) where the auxiliary ligands Lx are coumarin carboxylate derivatives bearing an oxylacetate moiety in the 6th or 7th position and...

Cited by 1 publication

References 68 publications

Design, Synthesis, Structural Insights, Tyrosinase Inhibition, and Sun Protection Factor of New Thiosemicarbazone Derivatives

Design, Synthesis, Structural Insights, Tyrosinase Inhibition, and Sun Protection Factor of New Thiosemicarbazone Derivatives

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