Chalcones: Promising therapeutic agents targeting key players and signaling pathways regulating the hallmarks of cancer

WalyEldeen, Amr Ahmed; Sabet, Salwa; El-Shorbagy, Haidan M.; Abdelhamid, Ismail A.; Ibrahim, Sherif

doi:10.1016/j.cbi.2022.110297

Cited by 51 publications

(24 citation statements)

References 195 publications

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“…In addition, 3-(furan-2-yl)-1H-pyrazoles (Andicsová et al 2018;Ryan et al 2020;Barus et al 2021) have been reported to have biologically interesting applications. Based on these findings, and in continuation of our study interest in bioactive heterocycle production (Mohamed et al 2017, 2021a, b, c, Sroor et al 2019Fathi et al 2021;Helmy et al 2021;Ragheb et al 2022;Salem et al 2022;Waly Eldeen et al 2022), we were inspired to synthesize the pyrazolyl-chalcones and evaluate their in vitro anti-cancer effectiveness against different human cancer cell lines with an emphasis on the novel two chalcones 7b, and 7c that proved strong and interesting cytotoxic effect against lung carcinoma (A549) cell line. To find their effect on the apoptotic process of cancer cells, many theoretical and experimental investigations were extensively performed.…”

Section: Introductionmentioning

confidence: 93%

Theoretical and molecular mechanistic investigations of novel (3-(furan-2-yl)pyrazol-4-yl) chalcones against lung carcinoma cell line (A549)

Mohamed

Ibrahim

Saddiq

et al. 2022

Naunyn-Schmiedeberg's Arch Pharmacol

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A new chalcone series has been developed that may be useful in the treatment of lung cancer. The new series was confirmed by the different spectral tools. MTT assay was used to detect the cytotoxic effect of the novel chalcones against lung cancer cell line (A549). Molecular docking studies were performed on the most two effective chalcones 7b and 7c. Different molecular techniques were utilized to study the activity and the effect of two chalcones 7b and 7c on apoptosis of A549 cell line.

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Section: Introductionmentioning

confidence: 93%

Theoretical and molecular mechanistic investigations of novel (3-(furan-2-yl)pyrazol-4-yl) chalcones against lung carcinoma cell line (A549)

Mohamed

Ibrahim

Saddiq

et al. 2022

Naunyn-Schmiedeberg's Arch Pharmacol

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“…Based on these facts and in continuation to our research interest in the synthesis of bioactive compounds [3,4,18,26–35] we report herein the synthesis of novel series of cyanoacrylamides linked to tetrahydrobenzo[ b ]thiophene moiety and test their cytotoxic activities against various cancer cell lines using MTT assay.…”

Section: Introductionmentioning

confidence: 99%

Cytotoxic Effect of New (E)‐2‐Cyano‐N‐(tetrahydrobenzo[b]thiophen‐2‐yl)acrylamide Derivatives: Down‐Regulation of RBL2 and STAT2 and Triggering of DNA Damage in Breast Carcinoma

Ibrahim,

Sroor,

Mahrous

et al. 2023

ChemistrySelect

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A novel series of 2‐cyano‐N‐(tetrahydrobenzo[b]thiophen‐2‐yl)acrylamide derivatives were synthesized and their structures were confirmed using several spectral tools. All compounds were subjected to MTT assay to elucidate their cytotoxic effect against human hepatocellular carcinoma (HEPG2), human Caucasian breast adenocarcinoma (MCF7), human pancreatic cancer cell line (PACA2), human prostate cancer cell line (PC3), and normal skin fibroblast (BJ1). Among them, the acrylamide derivatives 5, 10 and 14 exerted potent activities against MCF7 with IC50 values of 61.2, 66.4, and 55.3 μg/ml respectively. A molecular docking was performed to study the possibility of the molecular binding of these three compounds with the active site of signal transducer and activator of transcription 1 protein (STAT1). Gene expression analysis demonstrated the significant down‐regulation of RBL2 (RB transcriptional corepressor like 2) and STAT2 (Signal transducer and activator of transcription 2) in treated MCF7 cells and also showed the significant effect in down‐regulating KRAS (Ki‐ras2 Kirsten rat sarcoma viral oncogene homolog) and SMAD (Sma and Mad proteins) genes in PC3 cells. Comet assay revealed the best effect of Ethyl 2‐(2‐cyano‐3‐(3,4‐dimethoxyphenyl)acrylamido)‐4,5,6,7‐tetrahydrobenzo[b]thiophene‐3‐carboxylate in damaging the DNA of MCF7 cells (18.75±1.50 %). Also, DNA fragmentation was studied electrophoretically, which confirmed the results of the comet assay.

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“…The biological profile of chalcone attracted the attention of organic chemists worldwide to design and develop new chalcone derivatives (Rani et al 2019 ). Chalcones exhibited a variety of biological activities including antibacterial (Nanjundaswamy et al 2022 ), antifungal (Lahtchev et al 2008 ), anticancer (Mohamed et al 2012 , 2014 , 2018 , 2022 ; Tantawy et al 2019 ; Fathi et al 2021 ; Srilaxmi et al 2021 ; Helmy et al 2021 ; WalyEldeen et al 2022 , 2023 ; Kamel et al 2022 ; Sroor et al 2022 ) anti-inflammatory (Rojas et al 2003 ), antimalarial (Larsen et al 2005 ), and antiviral (Cheenpracha et al 2006 ). The mechanism of action for chalcones can be act via the α,β-unsaturated carbonyl moiety as Michael acceptor, thioredoxin reductase, and inhibition of microtubule formation (Menezes and Diederich 2019 ).…”

Section: Introductionmentioning

confidence: 99%

Novel eco-friendly [1,2,4]triazolo[3,4-a]isoquinoline chalcone derivatives efficiency against fungal deterioration of ancient Egyptian mummy cartonnage, Egypt

et al. 2023

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Fungal deterioration is one of the major factors that significantly contribute to mummy cartonnage damage. Isolation and molecular identification of thirteen fungal species contributing to the deterioration of ancient Egyptian mummy cartonnage located in El-Lahun regions, Fayoum government, Egypt was performed. The most dominant deteriorated fungal species are Aspergillus flavus (25.70%), Aspergillus terreus (16.76%), followed by A. niger (13.97%). A newly synthesized series of tetrahydro-[1,2,4]triazolo[3,4-a]isoquinoline chalcone derivatives were synthesized and evaluated for their antifungal activities in vitro against the isolated deteriorated fungal species (Aspergillus flavus, A. niger, A. terreus, Athelia bombacina, Aureobasidium iranianum, Byssochlamys spectabilis, Cladosporium cladosporioides, C. ramotenellum, Penicillium crustosum, P. polonicum, Talaromyces atroroseus, T. minioluteus and T. purpureogenus). The most efficient chalcone derivatives are new chalcone derivative numbers 9 with minimum inhibitory concentration (MIC) ranging from 1 to 3 mg/mL followed by chalcone derivatives number 5 with MIC ranging from 1 to 4 mg/mL.

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Chalcones: Promising therapeutic agents targeting key players and signaling pathways regulating the hallmarks of cancer

Cited by 51 publications

References 195 publications

Theoretical and molecular mechanistic investigations of novel (3-(furan-2-yl)pyrazol-4-yl) chalcones against lung carcinoma cell line (A549)

Theoretical and molecular mechanistic investigations of novel (3-(furan-2-yl)pyrazol-4-yl) chalcones against lung carcinoma cell line (A549)

Cytotoxic Effect of New (E)‐2‐Cyano‐N‐(tetrahydrobenzo[b]thiophen‐2‐yl)acrylamide Derivatives: Down‐Regulation of RBL2 and STAT2 and Triggering of DNA Damage in Breast Carcinoma

Novel eco-friendly [1,2,4]triazolo[3,4-a]isoquinoline chalcone derivatives efficiency against fungal deterioration of ancient Egyptian mummy cartonnage, Egypt

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