Discovery of 3-phenylquinolinylchalcone derivatives as potent and selective anticancer agents against breast cancers

Tseng, Chih‐Hua; Tzeng, Cherng‐Chyi; Hsu, Chen‐Chin; Cheng, C. C.; Yang, Chia‐Ning; Chen, Yeh‐Long

doi:10.1016/j.ejmech.2015.04.054

Cited by 29 publications

(10 citation statements)

References 38 publications

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“…In addition to the aforementioned chalcone hybrids, other hybrids, such as chalcone–ferrocene [ 95 , 96 , 97 ], chalcone–furan/thiophene hybrids [ 98 , 99 , 100 , 101 ], chalcone–pyridine/pyrimidine hybrids [ 102 , 103 , 104 , 105 , 106 ], chalcone–quinoline/quinolone hybrids [ 107 , 108 , 109 , 110 , 111 ], chalcone–quinoxaline/quinazolinone hybrids [ 112 , 113 , 114 ], chalcone-quinone hybrids [ 115 , 116 , 117 ], chalcone–triazine hybrids [ 118 , 119 ], and chalcone–dithiocarbamate hybrids [ 120 , 121 ] also showed certain anticancer activity.…”

Section: Strategies Employed To Produce Anticancer Chalconesmentioning

confidence: 99%

Chalcone Derivatives: Role in Anticancer Therapy

et al. 2021

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Chalcones (1,3-diaryl-2-propen-1-ones) are precursors for flavonoids and isoflavonoids, which are common simple chemical scaffolds found in many naturally occurring compounds. Many chalcone derivatives were also prepared due to their convenient synthesis. Chalcones as weandhetic analogues have attracted much interest due to their broad biological activities with clinical potentials against various diseases, particularly for antitumor activity. The chalcone family has demonstrated potential in vitro and in vivo activity against cancers via multiple mechanisms, including cell cycle disruption, autophagy regulation, apoptosis induction, and immunomodulatory and inflammatory mediators. It represents a promising strategy to develop chalcones as novel anticancer agents. In addition, the combination of chalcones and other therapies is expected to be an effective way to improve anticancer therapeutic efficacy. However, despite the encouraging results for their response to cancers observed in clinical studies, a full description of toxicity is required for their clinical use as safe drugs for the treatment of cancer. In this review, we will summarize the recent advances of the chalcone family as potential anticancer agents and the mechanisms of action. Besides, future applications and scope of the chalcone family toward the treatment and prevention of cancer are brought out.

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Section: Strategies Employed To Produce Anticancer Chalconesmentioning

confidence: 99%

Chalcone Derivatives: Role in Anticancer Therapy

et al. 2021

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“…Acid ceramidase can be inhibited by ceranib‐2 . Owing to its proapoptotic potential ceranib‐2 and related substances have been proposed for the treatment of malignancy …”

Section: Introductionmentioning

confidence: 99%

“…[46][47][48] Owing to its proapoptotic potential ceranib-2 and related substances have been proposed for the treatment of malignancy. 46,48,49 Even though lacking mitochondria, erythrocytes may similarly undergo suicidal death or eryptosis following exposure to ceramide 50 or sphingosine. 51 Eryptosis is characterized by cell shrinkage 52 and cell membrane scrambling with phosphatidylserine translocation to the cell surface.…”

Section: Introductionmentioning

confidence: 99%

Ceranib‐2‐induced suicidal erythrocyte death

Signoretto

Zierle

Bhuyan

et al. 2016

Cell Biochemistry & Function

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Ceramide is known to trigger apoptosis of nucleated cells and eryptosis of erythrocytes. Eryptosis is characterized by cell shrinkage and cell membrane scrambling with phosphatidylserine translocation to the erythrocyte surface. Besides ceramide, stimulators of eryptosis include increase of cytosolic Ca(2+) -activity ([Ca(2+) ]i ) and oxidative stress. Ceramide is degraded by acid ceramidase and inhibition of the enzyme similarly triggers apoptosis. The present study explored, whether ceramidase inhibitor Ceranib-2 induces eryptosis. Flow cytometry was employed to quantify phosphatidylserine-exposure at the cell surface from annexin-V-binding, cell volume from forward scatter, [Ca(2+) ]i from Fluo3-fluorescence, reactive oxygen species (ROS) from DCF dependent fluorescence, and ceramide abundance utilizing specific antibodies. Hemolysis was estimated from hemoglobin concentration in the supernatant. A 48 h exposure of human erythrocytes to Ceranib-2 significantly increased the percentage of annexin-V-binding cells (≥50 μM) and the percentage of hemolytic cells (≥10 μM) without significantly modifying forward scatter. Ceranib-2 significantly increased Fluo3-fluorescence, DCF fluorescence and ceramide abundance. The effect of Ceranib-2 on annexin-V-binding was not significantly blunted by removal of extracellular Ca(2+) . Ceranib-2 triggers phospholipid scrambling of the erythrocyte cell membrane, an effect at least in part due to increase of ceramide abundance and induction of oxidative stress, but not dependent on Ca(2+) entry. Copyright © 2016 John Wiley & Sons, Ltd.

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“…Moreover, cyclin B1, which is responsible for the regulation of the G 2 /M transition phase, has been found to be highly expressed in TNBCs as compared to other breast cancer subtypes as per a study investigating the expression levels of cyclin B1 in 1348 breast cancer patients [59]. Several studies have successfully synthesised chalcones with potent effects on apoptosis and cell cycle against TNBC cells [22,[60][61][62]. For instance, a group of pyrazolo[1,5-a]pyrimidines chalcone derivatives were prepared and tested for their effects on proliferation, cell cycle and apoptosis [60].…”

Section: Chalcone Derivatives As Potential Candidates For Tnbcs Treatmentioning

confidence: 99%

Targeting triple negative breast cancer heterogeneity with chalcones: a molecular insight

Alali

Moustafa

Khalil

2019

Journal of Drug Targeting

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Triple negative breast cancers (TNBCs) are aggressive heterogeneous cancers with not yet determined conventional targeted medication. Therefore, identification of new alternatives or improved treatment options to combat this deadly disease is highly needed. On the other hand, various derived products with chalcone scaffold were historically considered excellent candidates for the development of anticancer drugs. Chalcones unique chemical structure and their substantial biological activities in cancer cells make them an extremely attractive target for the treatment of several human carcinomas including TNBCs. This review highlights the promising therapeutic role of chalcones in TNBC management.

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Discovery of 3-phenylquinolinylchalcone derivatives as potent and selective anticancer agents against breast cancers

Cited by 29 publications

References 38 publications

Chalcone Derivatives: Role in Anticancer Therapy

Chalcone Derivatives: Role in Anticancer Therapy

Ceranib‐2‐induced suicidal erythrocyte death

Targeting triple negative breast cancer heterogeneity with chalcones: a molecular insight

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