Microwave assisted one-pot synthesis of novel 1,3,4-oxadiazole-imidazo[1',5':1,2]pyrrolo[3,4-d][1,2,3]triazoles as potent EGFR targeting Anticancer agents

Published: Jan. 1, 2025

Language: Английский

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Microwave-assisted one-pot synthesis of fused isoxazolo[4′,5′:3,4]pyrrolo[1,2-c]pyrimidines as potent anticancer agents: In vitro and in silico study

Tetrahedron Letters, Journal Year: 2025, Volume and Issue: 162, P. 155570 - 155570

Published: April 8, 2025

Language: Английский

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Synthesis and Anticancer Activity of Isoquinoline‐Imidazo[1,2‐a]Pyridine Linked Sulfonyl Derivatives

ChemistrySelect, Journal Year: 2025, Volume and Issue: 10(15)

Published: April 1, 2025

Abstract Several novel imidazo[1,2‐ a ]pyridine‐isoquinoline‐linked sulfonyl derivatives were designed and synthesized in this study. These subsequently assessed vitro for their inhibitory effects on EGFR kinases antiproliferative activity against two breast cancer cell lines. of the compounds demonstrated satisfactory efficacy comparison to primary agent, erlotinib. The most promising compounds, 6‐methoxy‐2‐methyl‐1‐(2‐phenyl‐6‐(1‐((3‐(trifluoromethyl)phenyl)sulfonyl)‐1,2,3,6‐tetrahydro pyridin‐4‐yl)imidazo[1,2‐a]pyridin‐3‐yl)‐1,2,3,4‐tetrahydro isoquinoline, 6‐methoxy‐2‐methyl‐1‐(2‐phenyl‐6‐(1‐((4‐(trifluoromethoxy) phenyl) sulfonyl)‐1,2,3,6‐tetrahydropyridin‐4‐yl)imidazo[1,2‐a]pyridin‐3‐yl)‐1,2,3,4‐tetrahydroisoquinoline, 6‐methoxy‐2‐methyl‐1‐(2‐phenyl‐6‐(1‐((3‐(trifluoromethoxy)phenyl)sulfonyl)‐1,2,3,6‐tetrahydropyridin‐4‐yl) imidazo[1,2‐a]pyridin‐3‐yl)‐1,2,3,4‐tetrahydroisoquinoline, exhibited exceptional anticancer MCF‐7 MDA‐MB‐231 lines, with IC 50 values ranging from 2.69 ± 0.24 7.64 0.15 µM. Subsequently results that above potent more efficacious than conventional medicine molecular interactions human epidermal growth factor receptor (EGFR) (PDB: 4HJO), which included co‐crystallized ligand (erlotinib) evaluated through silico docking studies. It was noted binding energies all higher those standard drug,

Language: Английский

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Design and Synthesis of Novel Quinoxaline-Piperazine Linked Isoxazole Conjugates: Anti-cancer Assessment, tyrosine kinase EGFR inhibitory activity, Molecular Docking and DFT Studies

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1321, P. 139839 - 139839

Published: Sept. 6, 2024

Language: Английский

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Halogen‐based quinazolin‐4(3H)‐one derivatives as MCF‐7 breast cancer inhibitors: Current developments and structure–activity relationship

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: 358(1)

Published: Nov. 13, 2024

Abstract Currently, cancer is a serious health challenge with predominance beyond restrictions. Breast remains one of the major contributors to cancer‐related morbidity and mortality in women. Chemotherapy continues be crucial treatment all variants cancer. Several antitumor drugs are presently different phases clinical trials, whereas many more have been approved for use. However, these potential cause adverse effects, certain individuals may become resistant them, which would eventually reduce drug's efficacy. Therefore, it essential discover, develop, improve newer anticancer drug molecules that could potentially inhibit proliferative pathways. In recent years, quinazolinone derivatives, specifically halogen‐substituted 4(3 H )‐quinazolinone, drawn attention as promising new class chemotherapeutic agents. addition, showed significant inhibition micromolar ranges when tested vitro against MCF‐7 cell line. this study aims emphasize intriguing versatility halogen atoms, providing an in‐depth summary highlighting developments properties halogenated )‐quinazolinones. It also features detailed discussion structure–activity relationship (SAR) various functional groups their interaction amino acid residues utilizing molecular docking studies. The intent foster novel discoveries can inspire innovative investigations domain. Hence, simplifies design development strategies by prolonging array pharmacologically active candidates.

Language: Английский

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The current landscape of 1,2,3‐triazole‐(fused) six‐membered nitrogen‐containing heteroaromatic ring hybrids with anticancer therapeutic potential

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: 358(1)

Published: Dec. 30, 2024

Cancer, characterized by uncontrolled growth and spread of abnormal cells potentially influencing almost all tissues in the body, is one most devastating lethal diseases throughout world. Chemotherapy principal approaches for cancer treatment, but multidrug resistance severe side effects represent main barriers to success therapy, creating a vital need develop novel chemotherapeutic agents. The 1,2,3-triazole moiety can be conveniently constructed "click chemistry" could exert diverse noncovalent interactions with various enzymes cells. Hence, fascinating anticancer pharmacophores. Moreover, also serve as powerful ligation tool complex molecular architectures increase efficacy lead molecules. Notably, 1,2,3-triazole-containing hybrids intriguing structural variations target different biological components simultaneously, highlighting their potential treatment eradication cancer. This review outlines current landscape 1,2,3-triazole-(fused) six-membered nitrogen-containing heteroaromatic ring hybrids, inclusive 1,2,3-triazole-quinazolines, 1,2,3-triazole-quinazolinones, 1,2,3-triazole-quinolines, 1,2,3-triazole-quinolones, 1,2,3-triazole-pyridines, 1,2,3-triazole-pyrimidines, therapeutic potential, explores mechanisms action, critical aspects design well structure-activity relationships (SARs), covering articles published from 2021 present, pave way development innovative efficient interventions therapy.

Language: Английский

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