Scorpionate ligand derived from 1-amino-9H-fluoren-9-ol and its metal (II) complexes as potential anticancer agents

Kumbar, Mahantesh; Patil, Sangamesh A.; Kinnal, Shivashankar M.; Jawoor, Shailaja S.; Shettar, Arun Kashivishwanath

doi:10.1016/j.cdc.2019.100226

Cited by 5 publications

(3 citation statements)

References 27 publications

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“…In conclusion, the cobalt scorpionate [Co(κ 3 -Tpm OH ) 2 ](NO 3 ) 2 (2) displayed a promising antiproliferative and anti-motogenic activity. Previous studies indicated that Co complexes can be more active that complexes with other metals [10,13,28]. These results are supported by the metabolomics alterations observed in cell adhesion-and membrane-structureassociated pathways.…”

Section: Discussionsupporting

confidence: 58%

Exploring the Mechanisms Behind the Anti-tumoral Effects of Model C-scorpionate Complexes

Pinheiro¹,

Camões²,

Ribeiro³

et al. 2023

Preprint

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The growing worldwide cancer incidence, coupled to the increasing occurrence of multidrug cancer resistance, requires a continuous effort towards the identification of new leads for cancer management. In this work, two C-scorpionate complexes, [FeCl2(κ3-Tpm)] (1) and [Co(κ3-TpmOH)2] (2), (Tpm = hydrotris(pyrazol-1-yl)methane and TpmOH = 2,2,2-tris(pyrazol-1-yl)ethanol), are studied as potential scaffolds for future anti-cancer drug development. Their cytotoxicity and cell migration inhibitory activity are analyzed, and an untargeted metabolomics approach is em-ployed to elucidate the biological processes significantly affected by these two complexes, using two tumoral cell lines (B16 and HCT116) and a non-tumoral cell line (HaCaT). While [FeCl2(κ3-Tpm)] did not display a significant cytotoxicity, [Co(κ3-TpmOH)2] was particularly cy-totoxic against the B16 cell line. While [Co(κ3-TpmOH)2] significantly inhibited cell migration in all tested cell lines, [FeCl2(κ3-Tpm)] displayed a mixed activity. From a metabolomics perspective, exposure to [FeCl2(κ3-Tpm)] is associated with changes in various metabolic pathways involving tyrosine, where iron-dependent enzymes are particularly relevant. On the other hand, [Co(κ3-TpmOH)2] is associated with dysregulation of cell adhesion and membrane structural pathways, suggesting its antiproliferative and anti-migration properties can be due to changes in the overall cellular adhesion mechanisms.

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Section: Discussionsupporting

confidence: 58%

Exploring the Mechanisms Behind the Anti-tumoral Effects of Model C-scorpionate Complexes

Pinheiro¹,

Camões²,

Ribeiro³

et al. 2023

Preprint

View full text Add to dashboard Cite

show abstract

“…In conclusion, the cobalt scorpionate [Co( κ 3 -Tpm OH ) 2 ](NO 3 ) 2 ( 2 ) displayed a promising antiproliferative and anti-motogenic activity. Previous studies indicated that Co complexes can be more active that complexes with other metals [ 10 , 13 , 28 ]. These results are supported by the metabolomics alterations observed in cell adhesion- and membrane-structure-associated pathways.…”

Section: Discussionmentioning

confidence: 99%

Exploring the Mechanisms behind the Anti-Tumoral Effects of Model C-Scorpionate Complexes

et al. 2023

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The growing worldwide cancer incidence, coupled to the increasing occurrence of multidrug cancer resistance, requires a continuous effort towards the identification of new leads for cancer management. In this work, two C-scorpionate complexes, [FeCl2(κ3-Tpm)] (1) and [Co(κ3-TpmOH)2](NO3)2 (2), (Tpm = hydrotris(pyrazol-1-yl)methane and TpmOH = 2,2,2-tris(pyrazol-1-yl)ethanol), were studied as potential scaffolds for future anticancer drug development. Their cytotoxicity and cell migration inhibitory activity were analyzed, and an untargeted metabolomics approach was employed to elucidate the biological processes significantly affected by these two complexes, using two tumoral cell lines (B16 and HCT116) and a non-tumoral cell line (HaCaT). While [FeCl2(κ3-Tpm)] did not display a significant cytotoxicity, [Co(κ3-TpmOH)2](NO3)2 was particularly cytotoxic against the HCT116 cell line. While [Co(κ3-TpmOH)2](NO3)2 significantly inhibited cell migration in all tested cell lines, [FeCl2(κ3-Tpm)] displayed a mixed activity. From a metabolomics perspective, exposure to [FeCl2(κ3-Tpm)] was associated with changes in various metabolic pathways involving tyrosine, where iron-dependent enzymes are particularly relevant. On the other hand, [Co(κ3-TpmOH)2](NO3)2 was associated with dysregulation of cell adhesion and membrane structural pathways, suggesting that its antiproliferative and anti-migration properties could be due to changes in the overall cellular adhesion mechanisms.

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“…9-Oxo-9H-fluorene-1-carboxylic acid is prepared from fluoranthene using potassium dichromate as an oxidizing agent as per the protocol reported in our previous publication [18]. Yield: 99%;…”

Section: Procedures For the Synthesis Of 9-oxo-9h-fluorene-1-carboxylimentioning

confidence: 99%

Anticancer activity studies of novel metal complexes of ligands derived from polycyclic aromatic compound via greener route

Kumbar

Patil

Toragalmath³

et al. 2020

Journal of Organometallic Chemistry

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Scorpionate ligand derived from 1-amino-9H-fluoren-9-ol and its metal (II) complexes as potential anticancer agents

Cited by 5 publications

References 27 publications

Exploring the Mechanisms Behind the Anti-tumoral Effects of Model C-scorpionate Complexes

Exploring the Mechanisms Behind the Anti-tumoral Effects of Model C-scorpionate Complexes

Exploring the Mechanisms behind the Anti-Tumoral Effects of Model C-Scorpionate Complexes

Anticancer activity studies of novel metal complexes of ligands derived from polycyclic aromatic compound via greener route

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