Design, synthesis, and anticancer assessment of structural analogues of ( E )-1-((3,4,5-trimethoxybenzylidene)amino)-4-(3,4,5-trimethoxyphenyl)imidazo[1,2- a ]quinoxaline-2-carbonitrile (6b), an imidazo[1,2- a ]quinoxaline-based non-covalent EGFR inhibitor

Manvendra Kumar; Kiran T. Patil; Pritam Maity; Joydeep Chatterjee; Tashvinder Singh; Gaurav Joshi; Sandeep Kumar Singh; Raj Kumar

doi:10.1039/d4md00237g

January 1, 2024RSC Medicinal ChemistryOpen Access

Design, synthesis, and anticancer assessment of structural analogues of ( E )-1-((3,4,5-trimethoxybenzylidene)amino)-4-(3,4,5-trimethoxyphenyl)imidazo[1,2- a ]quinoxaline-2-carbonitrile (6b), an imidazo[1,2- a ]quinoxaline-based non-covalent EGFR inhibitor

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Key Points

To design, synthesize, and evaluate structural analogues of an imidazo[1,2-a]quinoxaline template as non-covalent EGFR inhibitors for lung cancer treatment.
Designed and synthesized structural analogues based on the imidazo[1,2-a]quinoxaline scaffold derived from compound 6b.
Evaluated the synthesized compounds for their inhibitory activity against EGFR and their anticancer efficacy in lung cancer models.
Identified two lead analogues, designated 5a and 5l, that exhibited potent non-covalent EGFR inhibition.
Lead compounds 5a and 5l demonstrated strong anticancer activity against lung cancer cells.

Implication

Preclinical study demonstrates potent EGFR inhibition and anti-lung cancer activity by novel imidazoquinoxaline analogues, suggesting potential as non-covalent targeted therapies.

Abstract

Two lead compounds, 5a and 5l, designed on an imidazo[1,2- a ]quinoxaline template, emerged as potent EGFR inhibitors and anti-lung cancer agents.

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Cite This Study

Kumar et al. (2024) studied this question.

synapsesocial.com/papers/6ab3511fe229ba44ba385b66 https://doi.org/10.1039/d4md00237g

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Design, synthesis, and anticancer assessment of structural analogues of ( E )-1-((3,4,5-trimethoxybenzylidene)amino)-4-(3,4,5-trimethoxyphenyl)imidazo[1,2- a ]quinoxaline-2-carbonitrile (6b), an imidazo[1,2- a ]quinoxaline-based non-covalent EGFR inhibitor

Key Points

Implication

Abstract

Discussion

Cite This Study

Design, synthesis, and anticancer assessment of structural analogues of ( E )-1-((3,4,5-trimethoxybenzylidene)amino)-4-(3,4,5-trimethoxyphenyl)imidazo[1,2- a ]quinoxaline-2-carbonitrile (6b), an imidazo[1,2- a ]quinoxaline-based non-covalent EGFR inhibitor

Key Points

Implication

Abstract

Discussion

Cite This Study

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