Determination of anticancer potential of a novel pharmacologically active thiosemicarbazone derivative against colorectal cancer cell lines

Khan, Azmat Ali; Ahmad, Rehan; Alanazi, Amer M.; Alsaif, Nawaf A.; Abdullah, Maha; Wani, Tanveer A.; Bhat, M. A.

doi:10.1016/j.jsps.2022.03.011

Cited by 8 publications

(7 citation statements)

References 56 publications

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“…[28,30,31] TSCs can be functionalized with diverse bioactive or pharmacophoric groups and have been amply studied in medicinal chemistry [31,32] including clinical trials for multiple cancers (NCT02595879, NCT02688101, and NCT02433626). [19,33] Studies have shown that the anti-tumor activity of the thiosemicarbazones is due to their ability to act by multiple mechanisms of action, [34][35][36][37][38][39][40] such as inhibition of DNA synthesis, inhibition of cell proliferation, cell cycle, angiogenesis and metastasis, and modulation of signaling pathways. [39,40] These effects are produced by inhibition of targets such cysteine proteases, [33,37] ribonucleotide reductase, [36] cysteine proteases, [33,37] and/or the generation of reactive oxygen species (ROS).…”

Section: Introductionmentioning

confidence: 99%

“…[19,33] Studies have shown that the anti-tumor activity of the thiosemicarbazones is due to their ability to act by multiple mechanisms of action, [34][35][36][37][38][39][40] such as inhibition of DNA synthesis, inhibition of cell proliferation, cell cycle, angiogenesis and metastasis, and modulation of signaling pathways. [39,40] These effects are produced by inhibition of targets such cysteine proteases, [33,37] ribonucleotide reductase, [36] cysteine proteases, [33,37] and/or the generation of reactive oxygen species (ROS). [38] Thiosemicarbazones contain a soft sulfur donor atom able to easily coordinate to gold(I) centers.…”

Section: Introductionmentioning

confidence: 99%

“…Chemical structures of Auranofin (AF) and reported mono-and bimetallic god(I) compounds with anticancer activity. [36][37][38][39][40][41][42][43] ChemPlusChem bio reduced by parasite's enzymes to a nitro anion radical (NO 2…”

Section: Introductionmentioning

confidence: 99%

“… Chemical structures of Auranofin (AF) and reported mono‐ and bimetallic god(I) compounds with anticancer activity [36–43] …”

Section: Introductionmentioning

confidence: 99%

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5‐Nitrofuryl‐Containing Thiosemicarbazone Gold(I) Compounds: Synthesis, Stability Studies, and Anticancer Activity

Rodríguez‐Arce,

Gavrilov,

Alvite

et al. 2023

ChemPlusChem

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This work describes the synthesis of four gold(I) [AuClL] compounds containing chloro and biologically active protonated thiosemicarbazones based on 5‐nitrofuryl (L=HSTC). The stability of the compounds in dichloromethane, DMSO, and DMSO/culture media solutions was investigated by spectroscopy, cyclic voltammetry, and conductimetry, indicating the formation overtime of cationic monometallic [Au(HTSC)(DMSO)]± or [Au(HTSC)2]±, and/or dimeric species. Neutral [{Au(TSC)}2] species were obtained from one of the compounds in dichlomethane/n‐hexane solution and characterized by X‐ray crystallography revealing a Au−Au bond, and deprotonated thiosemicarbazone (TSC). The cytotoxicity of the gold compounds and thiosemicarbazone ligands was evaluated against selected cancer cell lines and compared to that of Auranofin. Studies of the most stable, cytotoxic, and selective compound on a renal cancer cell line (Caki‐1) demonstrated its relevant antimigratory and anti‐angiogenic properties, and preferential accumulation in the cell nuclei. Its mode of action seems to involve interaction with DNA, and subsequent cell death via apoptosis.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

“… Chemical structures of Auranofin (AF) and reported mono‐ and bimetallic god(I) compounds with anticancer activity [36–43] …”

Section: Introductionmentioning

confidence: 99%

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5‐Nitrofuryl‐Containing Thiosemicarbazone Gold(I) Compounds: Synthesis, Stability Studies, and Anticancer Activity

Rodríguez‐Arce,

Gavrilov,

Alvite

et al. 2023

ChemPlusChem

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“…In this context, cell cycle arrest is one of the main mechanisms that are involved in the development of anticancer compounds. The literature data highlighted that antiproliferative TSCs could affect cell cycle progression: some of them can induce G1/S [ 37 , 38 ] or G2/M [ 39 , 40 ] cell cycle block, while other compounds do not cause cell cycle arrest.…”

Section: Introductionmentioning

confidence: 99%

Modulation of Transcription Profile Induced by Antiproliferative Thiosemicarbazone Metal Complexes in U937 Cancer Cells

et al. 2023

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Since the discovery of cisplatin, the search for metal-based compounds with therapeutic potential has been a challenge for the scientific community. In this landscape, thiosemicarbazones and their metal derivatives represent a good starting point for the development of anticancer agents with high selectivity and low toxicity. Here, we focused on the action mechanism of three metal thiosemicarbazones [Ni(tcitr)2], [Pt(tcitr)2], and [Cu(tcitr)2], derived from citronellal. The complexes were already synthesized, characterized, and screened for their antiproliferative activity against different cancer cells and for genotoxic/mutagenic potential. In this work, we deepened the understanding of their molecular action mechanism using an in vitro model of a leukemia cell line (U937) and an approach of transcriptional expression profile analysis. U937 cells showed a significant sensitivity to the tested molecules. To better understand DNA damage induced by our complexes, the modulation of a panel of genes involved in the DNA damage response pathway was evaluated. We analyzed whether our compounds affected cell cycle progression to determine a possible correlation between proliferation inhibition and cell cycle arrest. Our results demonstrate that metal complexes target different cellular processes and could be promising candidates in the design of antiproliferative thiosemicarbazones, although their overall molecular mechanism is still to be understood.

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Reliable quality of R-phycoerythrin derived from Portieria hornemannii for effective antioxidant, antibacterial, and anticancer activity

Karuppannan,

Sivakumar,

Govindasamy

et al. 2024

Biomedical Engineering Advances

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Determination of anticancer potential of a novel pharmacologically active thiosemicarbazone derivative against colorectal cancer cell lines

Cited by 8 publications

References 56 publications

5‐Nitrofuryl‐Containing Thiosemicarbazone Gold(I) Compounds: Synthesis, Stability Studies, and Anticancer Activity

5‐Nitrofuryl‐Containing Thiosemicarbazone Gold(I) Compounds: Synthesis, Stability Studies, and Anticancer Activity

Modulation of Transcription Profile Induced by Antiproliferative Thiosemicarbazone Metal Complexes in U937 Cancer Cells

Reliable quality of R-phycoerythrin derived from Portieria hornemannii for effective antioxidant, antibacterial, and anticancer activity

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