Novel 2-substituted-quinoxaline analogs with potential antiproliferative activity against breast cancer: insights into cell cycle arrest, topoisomerase II, and EGFR activity

Salem, Manar G.; Abu El-ata, Sara A.; Elsayed, Elsherbiny H.; Mali, Suraj N.; Alshwyeh, Hussah Abdullah; Almaimani, Ghassan; Almaimani, Riyad A.; Almasmoum, Hussain A.; Altwaijry, Najla; Al-Olayan, Ebtesam; Saied, Essa M.; Youssef, Mohamed F.

doi:10.1039/d3ra06189b

Cited by 3 publications

(1 citation statement)

References 104 publications

(130 reference statements)

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“…Cell cycle analysis was performed using the propidium iodide (PI) flow cytometry kit (ab139418, Abcam, USA) by measuring the DNA content using a flow cytometer following the manufacturer's instructions. 43,53,54 Briefly, the CIR was dispersed in the cells, centrifugated at 500 g for 5 minutes, washed with 1× PBS, fixed with 66% ethanol on ice and resuspension of the cell pellet in 1× PBS followed by 100% ethanol. The subsequent PI staining procedure involved equilibrating the cells at room temperature, washing with 1× PBS and resuspending the cells in 1× PI + RNase staining solution.…”

Section: Methodsmentioning

confidence: 99%

Unveiling the multifaceted antiproliferative efficacy of Cichorium endivia root extract by dual modulation of apoptotic and inflammatory genes, inducing cell cycle arrest, and targeting COX-2

Alzahrani,

Hosny,

Mohamed

et al. 2024

RSC Adv.

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Section: Methodsmentioning

confidence: 99%

Unveiling the multifaceted antiproliferative efficacy of Cichorium endivia root extract by dual modulation of apoptotic and inflammatory genes, inducing cell cycle arrest, and targeting COX-2

Alzahrani,

Hosny,

Mohamed

et al. 2024

RSC Adv.

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The current landscape of coumarin hybrids with antibreast cancer therapeutic applications: An updated review

Wang,

Chen,

Huang

et al. 2024

Archiv der Pharmazie

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Globally, breast cancer (BC) has the highest prevalence among malignant diseases. BC is also the primary cause of death among women. Notably, BC morbidity has been increasing continuously at an approximate growth rate of 2.2% per year. Persistent BC is a major public health issue worldwide. Consequently, novel chemotherapeutic agents to combat this lethal disease should be developed urgently. Coumarins with interesting structural and mechanistic variations exhibit promising activity in several forms of BC, including BCs with multidrug resistance. In particular, coumarin hybrids composed of coumarin and one or more anti‐BC pharmacophores can target different biological components in BC cells simultaneously. Thus, coumarin hybrids are useful scaffolds that can help improve the anti‐BC efficacy of coumarins, reduce side effects, improve pharmacokinetics, minimize drug–drug interactions, and circumvent drug resistance. This review, in which articles published from 2020 to the present day have been evaluated, highlights the landscape of coumarin hybrids that exhibit therapeutic effects against breast cancer. These findings can aid further investigations on novel antibreast‐cancer therapeutics.

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Synthesis and antiproliferative evaluation of novel 3,5,8-trisubstituted coumarins against breast cancer

Salem,

Alqahtani,

Mali

et al. 2024

Future Medicinal Chemistry

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Aim: This study focused on designing and synthesizing novel derivatives of 3,5,8-trisubstituted coumarin. Results: The synthesized compounds, particularly compound 5, exhibited significant cytotoxic effects on MCF-7 cells, surpassing staurosporine, and reduced toxicity toward MCF-10A cells, highlighting potential pharmacological advantages. Further, compound 5 altered the cell cycle and significantly increased apoptosis in MCF-7 cells, involving both early (41.7-fold) and late stages (33-fold), while moderately affecting necrotic signaling. The antitumor activity was linked to a notable reduction (4.78-fold) in topoisomerase IIβ expression. Molecular modeling indicated compound 5‘s strong affinity for EGFR, human EGF2 and topoisomerase II proteins. Conclusion: These findings highlight compound 5 as a multifaceted antitumor agent for breast cancer.

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Novel 2-substituted-quinoxaline analogs with potential antiproliferative activity against breast cancer: insights into cell cycle arrest, topoisomerase II, and EGFR activity

Abstract: We reported a novel 2-coumarin-substituted-quinoxaline analogue (3b) with potential antiproliferative activity against MCF-7 breast cancer cells by inducing cell cycle arrest and targeting topoisomerase II, and EGFR activity.

Cited by 3 publications

References 104 publications

Unveiling the multifaceted antiproliferative efficacy of Cichorium endivia root extract by dual modulation of apoptotic and inflammatory genes, inducing cell cycle arrest, and targeting COX-2

Unveiling the multifaceted antiproliferative efficacy of Cichorium endivia root extract by dual modulation of apoptotic and inflammatory genes, inducing cell cycle arrest, and targeting COX-2

The current landscape of coumarin hybrids with antibreast cancer therapeutic applications: An updated review

Synthesis and antiproliferative evaluation of novel 3,5,8-trisubstituted coumarins against breast cancer

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