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核心技术专利：CN118964589B侵权必究
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Synthesis and cytotoxicity against tumor cells of pincer N-heterocyclic ligands and their transition metal complexes.

作者信息

Oulmidi Afaf, Radi Smaail, Idir Abderrazak, Zyad Abdelmajid, Kabach Imad, Nhiri Mohamed, Robeyns Koen, Rotaru Aurelian, Garcia Yann

机构信息

LCAE, Department of Chemistry, Faculty of Sciences, University Mohamed I BP 524 60 000 Oujda Morocco

Institute of Condensed Matter and Nanosciences, Molecular Chemistry, Materials and Catalysis (IMCN/MOST), Université catholique de Louvain Belgium.

出版信息

RSC Adv. 2021 Oct 27;11(55):34742-34753. doi: 10.1039/d1ra05918a. eCollection 2021 Oct 25.

DOI:10.1039/d1ra05918a
PMID:35494785
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9042687/
Abstract

The complexes: CoL (1), FeL (2), NiL (3) and [MnLCl] (4), with L = diethyl-1,1'-(pyridine-2,6-diyl)bis(5-methyl-1-pyrazole-3-carboxylate), were synthesized and fully characterized. Structural analysis revealed two distinct patterns influenced by the counter ions where L acts as a tridentate chelating ligand. The antitumor activity of L and L' (diethyl 2,2'-(pyridine-2,6-diylbis(5-methyl-1-pyrazole-3,1-diyl)) diacetate) as well as their metal complexes, was tested by the measurement of their cytostatic and cytotoxic properties towards the blood cancer mastocytoma cell line P815. We have also investigated their interactions with the antioxidant enzyme system. As a result, [MnL'Cl] (1') exhibited the strongest activity compared to reference cis-platin with no cytotoxicity towards normal cells PBMCs (Peripheral Blood Mononuclear Cells). On the other hand, the antioxidant enzyme activity showed that the efficiency of metal complex 1' against P815 tumor cells was the rise in the SOD activity and inhibition of CAT enzyme activity. This proof of concept study allows disclosure of a new class of molecules in cancer therapeutics.

摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/2243666bb9d4/d1ra05918a-f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/42b37c0efb8e/d1ra05918a-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/1b9f5e5e6852/d1ra05918a-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/935be847e25c/d1ra05918a-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/5300a06b5ff6/d1ra05918a-s4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/751cd9232342/d1ra05918a-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/e90b3ea3d04f/d1ra05918a-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/fa56bf3be113/d1ra05918a-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/5e288024aedc/d1ra05918a-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/75ec7e297e36/d1ra05918a-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/ec5d5c6e2915/d1ra05918a-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/8d6113af8181/d1ra05918a-f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/2243666bb9d4/d1ra05918a-f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/42b37c0efb8e/d1ra05918a-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/1b9f5e5e6852/d1ra05918a-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/935be847e25c/d1ra05918a-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/5300a06b5ff6/d1ra05918a-s4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/751cd9232342/d1ra05918a-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/e90b3ea3d04f/d1ra05918a-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/fa56bf3be113/d1ra05918a-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/5e288024aedc/d1ra05918a-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/75ec7e297e36/d1ra05918a-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/ec5d5c6e2915/d1ra05918a-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/8d6113af8181/d1ra05918a-f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62dc/9042687/2243666bb9d4/d1ra05918a-f8.jpg

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[3]
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[4]
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[5]
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本文引用的文献

[1]
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.

Eur J Med Chem. 2021-3-15

[2]
Zinc Complexes with Nitrogen Donor Ligands as Anticancer Agents.

Molecules. 2020-12-9

[3]
Synthesis, biological evaluation, and docking studies of new pyrazole-based thiourea and sulfonamide derivatives as inhibitors of nucleotide pyrophosphatase/phosphodiesterase.

Bioorg Chem. 2020-6

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New thiazole, pyridine and pyrazole derivatives as antioxidant candidates: synthesis, DFT calculations and molecular docking study.

Heliyon. 2020-1-9

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The synthesis and anticancer activity of 2-styrylquinoline derivatives. A p53 independent mechanism of action.

Eur J Med Chem. 2019-5-25

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Phytochemical Characterization, Antioxidant and In Vitro Cytotoxic Activity Evaluation of Subsp. Needles and Berries.

Molecules. 2019-1-30

[8]
The Anticancer Activities of Some Nitrogen Donor Ligands Containing bis-Pyrazole, Bipyridine, and Phenanthroline Moiety Using Docking Methods.

Bioinorg Chem Appl. 2018-6-4

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The Essential Element Manganese, Oxidative Stress, and Metabolic Diseases: Links and Interactions.

Oxid Med Cell Longev. 2018-4-5

[10]
Copper(II) complexes based on tripodal pyrazolyl amines: Synthesis, structure, magnetic properties and anticancer activity.

J Inorg Biochem. 2017-12-5

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