Synthesis and biological evaluation of quinoxaline derivatives as specific c-Met kinase inhibitors

Kim, Seung Chan; Boggu, Pulla Reddy; Yu, Hongkun; Ki, So Young; Jung, Jun Min; Kim, Yeon-Su; Park, Gi Min; Ho, Sang; Kim, In Su; Jung, Young Hoon

doi:10.1016/j.bmcl.2020.127189

Cited by 11 publications

(5 citation statements)

References 39 publications

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“…But compound 4 was the most potent one against MCF-7 (breast) cell line with IC50 value of 15.5 nM and against HCT-116 (colon) cell line with IC50 value of 9.8 nM. [20] as shown in…”

Section: Table (1 )mentioning

confidence: 82%

“…Also El-Adl in 2021 [18] arrested Compounds Cell line IC50 HepG2 8.4 HCT-116 21.4 MCF-7 24.5 [20] increased PDGFR receptor activity is crucial. The PDGF receptor tyrosine kinase is effectively inhibited by bicyclic quinoxaline derivatives [23] .…”

Section: Platelet-derived Growth Factor Receptor (Pdgfr) Inhibitorsmentioning

confidence: 99%

“…A crucial role in controlling cell development is played by the potent mitogen platelet-derived growth factor (PDGF). Tyrosine phosphorylation of natural substrates that function via a variety of pathways is a result of PDGF binding to its transmembrane receptor (PDGFR) [20] . Various PDGF isoforms have various interactions with the PDGF a-and b-receptors ( .…”

Section: Platelet-derived Growth Factor Receptor (Pdgfr) Inhibitorsmentioning

confidence: 99%

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Quinoxaline Derivatives Anti-Cancer Activities Through Protein Kinases Inhibition: A review

Fahmi,

nafie,

Youssef

2023

Advances in Environmental and Life Sciences

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Benzopyrazines, commonly known as quinoxaline derivatives, are a significant group of heterocyclic compounds. Due to the vast range of biological activities that quinoxalines exhibit, they have received a lot of interest. Derivatives of quinoxaline (benzopyrazine), which contain the pyrazoline ring structure, are a class of physiologically active compounds. They demonstrated broad range of biological activities; anticancer, anti-inflammatory, antibacterial, antidepressant, hypoglycemic, hypotensive, and antihistamic because of their ability to serve as protein kinase inhibitors, they are regarded as crucial starting point for anticancer medicines. Since quinoxalines have been shown to be selective ATP-competitive inhibitors of numerous kinases, including the Epidermal growth factor receptor EGFR/HER2 inhibitors, vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), C-Met kinase inhibitor, Janus kinase receptor (JAK-2) and cyclin dependent kinase (CDK1,2,4,6). Quinoxaline derivatives' chemistry and their possible anti-protein kinase effects are the main topics of this paper.Anticancer / Kinase inhibitors / Quinoxalines derivatives.

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“…But compound 4 was the most potent one against MCF-7 (breast) cell line with IC50 value of 15.5 nM and against HCT-116 (colon) cell line with IC50 value of 9.8 nM. [20] as shown in…”

Section: Table (1 )mentioning

confidence: 82%

Section: Platelet-derived Growth Factor Receptor (Pdgfr) Inhibitorsmentioning

confidence: 99%

Section: Platelet-derived Growth Factor Receptor (Pdgfr) Inhibitorsmentioning

confidence: 99%

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Quinoxaline Derivatives Anti-Cancer Activities Through Protein Kinases Inhibition: A review

Fahmi,

nafie,

Youssef

2023

Advances in Environmental and Life Sciences

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“…Although 16 lacked a hydrogen bond with P1158, the lost activity can be compensated by the increased hydrophobic interaction of the quinoline group with M1211 . Other examples, such as pyridine-2(1 H )-one ( 17 ), pyridazin-3-amine ( 18 ), furan[3,2- c ]pyridin-6-amine ( 19 ), and quinoxaline ( 20 ) were used as alternative hinge binders.…”

Section: Small Molecule Inhibitors Of Metmentioning

confidence: 99%

Targeting MET: Discovery of Small Molecule Inhibitors as Non-Small Cell Lung Cancer Therapy

Wang

2023

J. Med. Chem.

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MET has been considered as a promising drug target for the treatment of MET-dependent diseases, particularly non-small cell lung cancer (NSCLC). Small molecule MET inhibitors with mainly three types of binding modes (Ia/Ib, II, and III) have been developed. In this Review, we provide an overview of the structural features, activation mechanism, and dysregulation pathway of MET and summarize progress on the development and discovery strategies utilized for MET inhibitors as well as mechanisms of acquired resistance to current approved inhibitors. The insights will accelerate discovery of new generation MET inhibitors to overcome clinical acquired resistance.

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“…Spiroindeno [1,2]quinoxaline-11,4'-pyrans are biologically active compounds consisting of quinoxaline, indole, and pyran pharmacophores and a spiro center. Extensive pharmaceutical activities have been detected for these structural moieties such as anti-tuberculosis [13], anti-depressant [14], antibacterial [15,16], anti-fungal [17], anti-cancer [18], kinase inhibitors [19,20], anti-tumor [21,22], antioxidant [23] and anti-in ammatory [24] properties [25][26][27][28][29]. Furthermore, the medical effects of spiro compounds have been con rmed in the treatment of tuberculosis, cancer, HIV, bacterial and fungal infections [30].…”

Section: Introductionmentioning

confidence: 99%

The application of a metal-organic framework based on copper (MOF-199) and its modified form (G@MOF-199) in the four-component synthesis of spiro indenoquinoxaline derivatives

Hojati

Amiri

khaleghinasab

2023

Preprint

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The metal-organic framework based on copper (MOF-199) has been synthesized and loaded on the surface of the graphene sheets to give G@MOF-199 nanocomposite and characterized using FT-IR, SEM, and TEM analyses. The catalytic application of MOF-199 and its modified form (G@MOF-199) was investigated in the four-component synthesis of 2'-aminospiro[indeno[1,2-b]quinoxaline-11,4' -[4'H] pyran]-3'-carbonitrile derivatives and compared together. It was found that the G@MOF-199 nanocomposite is reusable and its catalytic activity is more than MOF-199. High yields, short reaction times, mild reaction conditions, and easy work-up procedure, in combination with stability, efficiency, and non-toxicity of the catalysts are noteworthy advantages of both methods.

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Synthesis and biological evaluation of quinoxaline derivatives as specific c-Met kinase inhibitors

Cited by 11 publications

References 39 publications

Quinoxaline Derivatives Anti-Cancer Activities Through Protein Kinases Inhibition: A review

Quinoxaline Derivatives Anti-Cancer Activities Through Protein Kinases Inhibition: A review

Targeting MET: Discovery of Small Molecule Inhibitors as Non-Small Cell Lung Cancer Therapy

The application of a metal-organic framework based on copper (MOF-199) and its modified form (G@MOF-199) in the four-component synthesis of spiro indenoquinoxaline derivatives

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