Advances in chalcone-based anticancer therapy: mechanisms, preclinical advances, and future perspectives DOI

Shefali Chowdhary,

Preeti Preeti,

Shekhar Shekhar

et al.

Expert Opinion on Drug Discovery, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 2, 2024

Introduction Cancerremains a leading cause of death worldwide with traditional treatments likechemotherapy, and radiotherapy becoming less effective due to multidrugresistance (MDR). This highlights the necessity for novel chemotherapeuticslike chalcone based compounds, which demonstrate broad anti-cancer propertiesand target multiple pathways. These compounds hold promise improving cancertreatment outcomes compared existing therapies.

Language: Английский

Design, Synthesis and Evaluation of Quinazoline-Chalcone Hybrids as Inducers of Cell-Cycle Arrest and Apoptosis in Breast Cancer via DNA Damage and CDK2/ATR Inhibition DOI Creative Commons
Giulia Rodrigues Stringhetta, Eduardo Bustos Mass, Izabela Natália Faria Gomes

et al.

European Journal of Medicinal Chemistry Reports, Journal Year: 2025, Volume and Issue: unknown, P. 100250 - 100250

Published: Feb. 1, 2025

Language: Английский

Citations

0
Structure-Based Design of New LSD1/EGFRL858R/T790M Dual Inhibitors for Treating EGFR Mutant NSCLC Cancers DOI
Jingya Zhang, Pengxing He, Wenwen Wang

et al.

Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 27, 2025

Epigenetic changes, such as LSD1 dysregulation, contribute to acquired resistance in EGFR mutant NSCLCs and reduce the effectiveness of current therapeutics. To address challenges, we herein reported structure-based design new LSD1/EGFR dual inhibitors, which ZJY-54 represents shortlisted lead compound with high potency, selectivity, unique modes action (namely irreversibly binding but reversibly LSD1). effectively inhibited growth both parent- TKI-resistant NSCLC cells. In H1975 cells, induced accumulation H3K4me2 H3K9me2, well phosphorylation signaling. showed favorable PK profiles tumor xenograft model. best-in-class inhibitor warrants further preclinical development for treating NSCLCs. These findings highlight therapeutic potential inhibitors drug-resistant cancers where were dysregulated.

Language: Английский

Citations

0
Novel 2‐[thio]acetamide linked quinazoline/1,2,4‐triazole/chalcone hybrids: Design, synthesis, and anticancer activity as EGFR inhibitors and apoptotic inducers DOI
Ahmed S. Abdelkhalek, Hend Kothayer, Moustafa K. Soltan

et al.

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: 357(7)

Published: April 9, 2024

Novel triazoloquinazolines carrying the 2-[thio]acetamide entity (4 and 5a-d) triazoloquinazoline/chalcone hybrids incorporating linker (8a-b 9a-f) were developed as anticancer candidates. NCI screening of synthesized compounds at 10 μM concentration displayed growth inhibition not only up to 99.74% observed for 9a but also a lethal effect could be achieved stated 9c (RPMI-8226 HCT-116) 8b, 9a, 9e on HCT-116 cell line. The antiproliferative activity was determined chalcone series three lines: RPMI-8226, HCT-116, MCF-7. Compounds 9b, 9f most active ones. To understand mechanistic study, inhibitory epidermal factor receptor (EGFR) kinase evaluated. results that compound 8b (IC

Language: Английский

Citations

2
Advances in chalcone-based anticancer therapy: mechanisms, preclinical advances, and future perspectives DOI

Shefali Chowdhary,

Preeti Preeti,

Shekhar Shekhar

et al.

Expert Opinion on Drug Discovery, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 2, 2024

Introduction Cancerremains a leading cause of death worldwide with traditional treatments likechemotherapy, and radiotherapy becoming less effective due to multidrugresistance (MDR). This highlights the necessity for novel chemotherapeuticslike chalcone based compounds, which demonstrate broad anti-cancer propertiesand target multiple pathways. These compounds hold promise improving cancertreatment outcomes compared existing therapies.

Language: Английский

Citations

1