Novel quinazoline-based EGFR kinase inhibitors: A review focussing on SAR and molecular docking studies (2015-2019)

Bhatia, Parth; Sharma, Vrinda; Alam, Ozair; Manaithiya, Ajay; Alam, Pravej; Kahksha,; Alam, Tauquir; Imran, Mohd

doi:10.1016/j.ejmech.2020.112640

Cited by 75 publications

(65 citation statements)

References 118 publications

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“…The Epidermal Growth Factor Receptor (EGFR) overexpression is recognized as a driver mechanism in the initiation, progression, and therapy resistance of several carcinomas such as lung, breast, and pancreatic cancers [ 44 ], added the interaction HOXB7/EGFR promoter region already demonstrated [ 25 ]. EGFR is also an important target for multiple chemotherapeutic regimens [ 45 ].…”

Section: Discussionmentioning

confidence: 99%

HOXB7 Overexpression Leads Triple-Negative Breast Cancer Cells to a Less Aggressive Phenotype

et al. 2021

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HOX genes appear to play a role in breast cancer progression in a molecular subtype-dependent way. The altered expression of HOXB7, for example, was reported to promote breast cancer progression in specific subtypes. Here we induced HOXB7 overexpression in MDA-MB-231 cells, a cellular model of the Triple-Negative breast cancer molecular subtype, and evaluated the phenotypic changes in cell viability, morphogenesis, migration, invasion, and colony formation. During the phenotypic characterization of the HOXB7-overexpressing cells, we consistently found less aggressive behavior represented by lower cell viability, inhibition of cell migration, invasion, and attachment-independent colony formation capacities added to the more compact and organized spheroid growth in 3D cultures. We then evaluated the expression of putative downstream targets and their direct binding to HOXB7 comparing ChIP-qPCR data generated from HOXB7-overexpressing cells and controls. In the manipulated cells, we found enriched biding of HOXB7 to CTNNB1, EGFR, FGF2, CDH1, DNMT3B, TGFB2, and COMMD7. Taken together, these results highlight the plasticity of the HOXB7 function in breast cancer, according to the cellular genetic background and expression levels, and provide evidence that in Triple-Negative breast cancer cells, HOXB7 overexpression has the potential to promote less aggressive phenotypes.

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Section: Discussionmentioning

confidence: 99%

HOXB7 Overexpression Leads Triple-Negative Breast Cancer Cells to a Less Aggressive Phenotype

et al. 2021

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“…ZrOCl2. 8H2O, CeO2 and H2O2 proved to be inefficient oxidants in the C-H arylation of quinazoline 3-oxides (Table 1, [4][5][6]. The reaction without oxidant did not produce any product after 44 h heating in acetonitrile.…”

Section: Resultsmentioning

confidence: 99%

“…1 The pharmacological activities of quinazoline based scaffolds include anti-cancer, anti-microbial, anticonvulsant, and anti-hyperlipidemic. [2][3][4][5] A vast number of quinazoline derivatives have been synthesized to provide synthetic drugs and to design more effective medicines (gefitinib, erlotinib, raltitrexed, prazosin, doxazosin etc.) Some developments in the environmentally benign, green, and efficient synthetic protocols (in most cases) to access quinazoline and quinazolinone derivatives from cheap and readily available commercial feedstocks are reviewed.…”

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confidence: 99%

Mn(OAc)3 Induced C-4 Arylations of Quinazoline 3-Oxides with Arylboronic Acids

2021

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The use of manganese triacetate as an oxidant component in the C-4 arylations of 2-aryl-quinazoline 3-oxides with arylboronic acids is reported. The new protocol was applied to prepare new 2,4-diarylated quinazoline 3-oxides in good to high yields. The method was shown to tolerate various substituents on both aromatic rings, and no complications as deoxygenation and rearrangement to quinazolin-4(3H)-one was observed.

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“…An important part of tumor biology research is an intense search for, and design of, antitumor drugs effective in inhibiting the activity of tyrosine kinases and which come with recommended physico-chemical properties that determine pharmacokinetic processes. The following are examples of tyrosine kinase inhibitors: pyrrole, morpholine, and urea moieties ( Figure 2 : 11–13) ( Bhatia et al, 2020 ; Yang et al, 2021 ).…”

Section: Antitumor Effects Of Quinazoline Derivativesmentioning

confidence: 99%

Quinazoline Derivatives as Potential Therapeutic Agents in Urinary Bladder Cancer Therapy

et al. 2021

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Cancer diseases remain major health problems in the world despite significant developments in diagnostic methods and medications. Many of the conventional therapies, however, have limitations due to multidrug resistance or severe side effects. Bladder cancer is a complex disorder, and can be classified according to its diverse genetic backgrounds and clinical features. A very promising direction in bladder cancer treatment is targeted therapy directed at specific molecular pathways. Derivatives of quinazolines constitute a large group of chemicals with a wide range of biological properties, and many quinazoline derivatives are approved for antitumor clinical use, e.g.,: erlotinib, gefitinib, afatinib, lapatinib, and vandetanib. The character of these depends mostly on the properties of the substituents and their presence and position on one of the cyclic compounds. Today, new quinazoline-based compounds are being designed and synthesized as potential drugs of anticancer potency against bladder cancers.

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Novel quinazoline-based EGFR kinase inhibitors: A review focussing on SAR and molecular docking studies (2015-2019)

Cited by 75 publications

References 118 publications

HOXB7 Overexpression Leads Triple-Negative Breast Cancer Cells to a Less Aggressive Phenotype

HOXB7 Overexpression Leads Triple-Negative Breast Cancer Cells to a Less Aggressive Phenotype

Mn(OAc)3 Induced C-4 Arylations of Quinazoline 3-Oxides with Arylboronic Acids

Quinazoline Derivatives as Potential Therapeutic Agents in Urinary Bladder Cancer Therapy

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