Gold(III) complexes with thiosemicarbazone ligands: insights into their cytotoxic effects on lung cancer cells

Scaccaglia, Mirco; Pinelli, Silvana; Manini, Luca; Ghezzi, Benedetta; Nicastro, Maria; Heinrich, Julian; Kulak, Nora; Mozzoni, Paola; Pelosi, Giorgio; Bisceglie, Franco

doi:10.1016/j.jinorgbio.2023.112438

Cited by 4 publications

(1 citation statement)

References 30 publications

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“…Salicylaldehyde or 2-hydroxy-benzaldehyde (saloH) is an organic compound found in the defensive secretion of some leaf beetle species [3]. Salicylaldehyde-based compounds are derivatives of saloH formed either by reactions through the carbonyl group leading to novel classes of compounds bearing the salicylaldehyde scaffold, such as Schiff bases [4][5][6][7], hydrazides [8,9], hydrazones [10][11][12][13], or thiosemicarbazones [14][15][16], or by the insertion of diverse substituents on one or more positions of the aromatic leading to substituted salicylaldehydes.…”

Section: Introductionmentioning

confidence: 99%

Coordination Compounds of Nickel(II) with 3,5–Dibromo–Salicylaldehyde: Structure and Interaction with Biomolecules

Psarras,

Zianna,

Hatzidimitriou

et al. 2024

Inorganics

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Three neutral nickel(II) complexes of 3,5–dibromo–salicylaldehyde (3,5–diBr–saloH) were synthesized in the presence or absence of 1,10–phenanthroline (phen) or its derivative 2,9–dimethyl–1,10–phenanthroline (neoc) as co–ligands, namely [Ni(3,5–diBr–salo)2(neoc)] (complex 1), [Ni(3,5–diBr–salo)2(phen)] (complex 2) and [Ni(3,5–diBr–salo)2(H2O)2] (complex 3), and were characterized by various techniques. The crystal structure of [Ni(3,5–diBr–salo)2(neoc)] was determined by single-crystal X-ray crystallography. According to employed studying techniques, the complexes interact tightly with calf-thymus DNA by an intercalative fashion. Furthermore, compounds 1–3 bind tightly and reversibly to human and bovine serum albumin.

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Section: Introductionmentioning

confidence: 99%

Coordination Compounds of Nickel(II) with 3,5–Dibromo–Salicylaldehyde: Structure and Interaction with Biomolecules

Psarras,

Zianna,

Hatzidimitriou

et al. 2024

Inorganics

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Recent development of Schiff-base metal complexes as therapeutic agents for lung cancer

Jiang,

Su,

Zhong

et al. 2024

Journal of Molecular Structure

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Design, synthesis, in vitro and in silico studies of novel piperidine derived thiosemicarbazones as inhibitors of dihydrofolate reductase

Aftab,

Ullah,

Khan

et al. 2024

Sci Rep

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Dihydrofolate reductase (DHFR), an essential enzyme in folate metabolism, presents a promising target for drug development against various diseases, including cancer and tuberculosis. Herein, we present an integrated approach combining in vitro biochemical assays with in silico molecular docking analysis to evaluate the inhibitory potential of 4-piperidine-based thiosemicarbazones 5 ( a-s ) against DHFR. In our in vitro study, a novel series of 4-piperidine-based thiosemicarbazones 5 ( a-s ) were assessed for their inhibitory activity against DHFR enzyme. The synthesized compounds 5 ( a-s ) exhibited potent inhibition with IC 50 values in the range of 13.70 ± 0.25 µM to 47.30 ± 0.86 µM. Among all the derivatives 5p displayed highest inhibitory activity. Simultaneously, in silico analysis were performed and compared with standard drug (Methotrexate) to predict the binding affinity and interaction pattern of synthesized compounds with DHFR active site. SAR analysis was done to elucidate how structural modifications impact compound’s biological activity, guiding the rational design of potent and selective drug candidates for targeted diseases. These findings may provide a comprehensive assessment of 4-piperdine-based thiosemicarbazones as DHFR inhibitors and contribute to the development of novel therapeutics targeting DHFR-associated diseases. Supplementary Information The online version contains supplementary material available at 10.1038/s41598-024-72858-2.

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Gold(III) complexes with thiosemicarbazone ligands: insights into their cytotoxic effects on lung cancer cells

Cited by 4 publications

References 30 publications

Coordination Compounds of Nickel(II) with 3,5–Dibromo–Salicylaldehyde: Structure and Interaction with Biomolecules

Coordination Compounds of Nickel(II) with 3,5–Dibromo–Salicylaldehyde: Structure and Interaction with Biomolecules

Recent development of Schiff-base metal complexes as therapeutic agents for lung cancer

Design, synthesis, in vitro and in silico studies of novel piperidine derived thiosemicarbazones as inhibitors of dihydrofolate reductase

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