Exploration of 3,4-unsubstituted coumarins as thioredoxin reductase 1 inhibitors for cancer therapy

Nikitjuka, A.; Ozola, M.; Jackevica, L.; Bobrovs, R.; Žalubovskis, R.

doi:10.1039/d3ob01522j

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Org. Biomol. Chem.

2023

DOI: 10.1039/d3ob01522j

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Exploration of 3,4-unsubstituted coumarins as thioredoxin reductase 1 inhibitors for cancer therapy

A. Nikitjuka,

M. Ozola,

L. Jackevica

et al.

Abstract: The synthesis and estimation of the structure–activity relationship of a range of 3,4-unsubstituted coumarins are described. Natural-like scaffold of coumarin remains a privileged source of potential TrxR1 inhibitors for anticancer application.

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2024

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Dual Inhibitors of P-gp and Carbonic Anhydrase XII (hCA XII) against Tumor Multidrug Resistance with Piperazine Scaffold

Braconi,

Riganti,

Parenti

et al. 2024

Molecules

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A new series of piperazine derivatives were synthesized and studied with the aim of obtaining dual inhibitors of P-glycoprotein (P-gp) and carbonic anhydrase XII (hCA XII) to synergistically overcome the P-gp-mediated multidrug resistance (MDR) in cancer cells expressing the two proteins, P-gp and hCA XII. Indeed, these hybrid compounds contain both P-gp and hCA XII binding groups on the two nitrogen atoms of the heterocyclic ring. All compounds showed good inhibitory activity on each protein (P-gp and hCA XII) studied individually, and many of them showed a synergistic effect in the resistant HT29/DOX and A549/DOX cell lines which overexpress both the target proteins. In particular, compound 33 displayed the best activity by enhancing the cytotoxicity and intracellular accumulation of doxorubicin in HT29/DOX and A549/DOX cells, thus resulting as promising P-gp-mediated MDR reverser with a synergistic mechanism. Furthermore, compounds 13, 27 and 32 induced collateral sensitivity (CS) in MDR cells, as they were more cytotoxic in resistant cells than in the sensitive ones; their CS mechanisms were extensively investigated.

show abstract

Dual Inhibitors of P-gp and Carbonic Anhydrase XII (hCA XII) against Tumor Multidrug Resistance with Piperazine Scaffold

Braconi,

Riganti,

Parenti

et al. 2024

Molecules

View full text Add to dashboard Cite

show abstract

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Exploration of 3,4-unsubstituted coumarins as thioredoxin reductase 1 inhibitors for cancer therapy

Abstract: The synthesis and estimation of the structure–activity relationship of a range of 3,4-unsubstituted coumarins are described. Natural-like scaffold of coumarin remains a privileged source of potential TrxR1 inhibitors for anticancer application.

Cited by 1 publication

References 34 publications

Dual Inhibitors of P-gp and Carbonic Anhydrase XII (hCA XII) against Tumor Multidrug Resistance with Piperazine Scaffold

Dual Inhibitors of P-gp and Carbonic Anhydrase XII (hCA XII) against Tumor Multidrug Resistance with Piperazine Scaffold

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