Design, synthesis and biological evaluation of new series of hexahydroquinoline and fused quinoline derivatives as potent inhibitors of wild-type EGFR and mutant EGFR (L858R and T790M)

“…Results demonstrated that compound 66 a highlighted the remarkable activity against EGFR WT , EGFR L858R and EGFR T790M with IC 50 value of 0.083, 0.053 and 0.026 μM respectively. Cell cycle research demonstrated that 66a promoted G2/M and pre‐G1 cell cycle arrest in the tested cancer cells [138] …”

Section: Recent Development Of Different Nitrogen Containing Derivati...mentioning

confidence: 97%

Nitrogen‐Containing Heterocyclic Scaffolds as EGFR Inhibitors: Design Approaches, Molecular Docking, and Structure‐Activity Relationships

Pal¹,

Teli²,

Matada³

et al. 2023

ChemistrySelect

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proved to be the magical weapon in designed and discovery of synthetic molecules as they acquired comprehensive range of pharmacological properties. In recent year (2018-2022) Nheterocyclic derivatives were uncovered as the potential EGFR TKIs. The present review summarised the research progress of EGFR TKIs to dazed the limitations of currently accessible drugs by consecrating, anatomy, mutation of EGFR, and its role in different types of cancer. The review highlights the medicinal chemistry prospective emphasising about the designing strategies, docking studies, biological evaluation, selectivity and structural activity relationship of N-heterocyclic compounds. Our review will support the medicinal chemists in direction for the development of novel N-heterocyclic based EGFR TKIs.

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“…Compounds containing a quinolinone moiety are commonly evaluated in drug discovery efforts because of the wide range of pharmacological activities they exhibit. These types of compounds remain attractive as potential scaffolds for incorporation into pharmaceutical agents as they display properties such as antimicrobial 10,11 antiproliferative, 12 anticancer, 13,14 antitubercular, 15 and antioxidant 16 activities. Selected quinolinone-containing structures exhibiting biological activity are presented in Figure 2.…”

Section: Frommentioning

confidence: 99%

Synthesis of Hexahydroquinoline-3-carboxamide Derivatives and Their HIV-1 Antiviral Activity

Bode¹,

Coyanis²,

Mohlala³

et al. 2022

HETEROCYCLES

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Computational modelling was used to identify scaffolds with the potential to disrupt the interaction between HIV-1 integrase and lens epitheliumderived growth factor (HIV-1-IN-LEDGF/p75). Virtual screening of commercial library collections led to the identification of N-(4-chlorophenyl)-7,7-dimethyl-2,5dioxo-1,2,5,6,7,8-hexahydroquinoline-3-carboxamide as a promising candidate.The synthesis of this compound and its derivatives involved the reaction of the corresponding carboxylic acid derivatives with aniline in the presence of coupling agent carbonyldiimidazole (CDI). This gave rise to N-2,5-dioxo-1,2,5,6,7,8-hexahydroquinoline-3-carboxamides in yields of 71-85% . These compounds were found to be non-toxic in an MT4 cell line at 100 μM and were subsequently evaluated for antiviral activity in infected MT4 cells at a single dose concentration of 100 μM.

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Design, synthesis and biological evaluation of new series of hexahydroquinoline and fused quinoline derivatives as potent inhibitors of wild-type EGFR and mutant EGFR (L858R and T790M)

Cited by 18 publications

References 76 publications

Quinoline–hydrazone hybrids as dual mutant EGFR inhibitors with promising metallic nanoparticle loading: rationalized design, synthesis, biological investigation and computational studies

Quinoline–hydrazone hybrids as dual mutant EGFR inhibitors with promising metallic nanoparticle loading: rationalized design, synthesis, biological investigation and computational studies

Nitrogen‐Containing Heterocyclic Scaffolds as EGFR Inhibitors: Design Approaches, Molecular Docking, and Structure‐Activity Relationships

Synthesis of Hexahydroquinoline-3-carboxamide Derivatives and Their HIV-1 Antiviral Activity

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