Combination of radial distribution functions as structural descriptors with ligand-receptor interaction information in the QSAR study of some 4-anilinoquinazoline derivatives as potent EGFR inhibitors
Sign Up to like & getrecommendations! Published in 2020 at "Structural Chemistry"
DOI: 10.1007/s11224-020-01505-z
Abstract: In this paper, we report the use of a mixture of radial distribution functions (RDFs) and molecular docking descriptors (MDDs), as a new group of descriptors, to construct a predictive quantitative structure-activity relationship (QSAR) model.… read more here.
Keywords: egfr inhibitors; model; radial distribution; receptor ... See more keywords
EGF receptor inhibitors comprehensively suppress hepatitis B virus by downregulation of STAT3 phosphorylation
Sign Up to like & getrecommendations! Published in 2020 at "Biochemistry and Biophysics Reports"
DOI: 10.1016/j.bbrep.2020.100763
Abstract: Current antiviral therapy can not cure chronic hepatitis B virus (HBV) infection or eliminate the risk of hepatocellular carcinoma. The licensed epidermal growth factor receptor (EGFR) inhibitors have found to inhibit hepatitis C virus replication… read more here.
Keywords: egfr inhibitors; hbv; hepatitis virus; stat3 phosphorylation ... See more keywords
Synthesis and anti-proliferative activity of some new quinoline based 4,5-dihydropyrazoles and their thiazole hybrids as EGFR inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.10.038
Abstract: Quinoline derivatives 2, 3, quinolinyl based pyrazolines 4a,b, 5 and quinolinyl pyrazolinyl thiazole hybrids 6a-d, 7a-c and 8a-d were synthesized and screened for their anti-proliferative activity against MCF-7, HeLa and DLD1 cancer cell lines as… read more here.
Keywords: anti proliferative; egfr inhibitors; quinoline; thiazole hybrids ... See more keywords
A review on progression of epidermal growth factor receptor (EGFR) inhibitors as an efficient approach in cancer targeted therapy.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.103811
Abstract: The identification of molecular agents inhibiting specific functions in cancer cells progression is considered as one of the most successful plans in cancer treatment. The epidermal growth factor receptor (EGFR) over-activation is observed in a… read more here.
Keywords: factor receptor; egfr inhibitors; growth factor; cancer ... See more keywords
Allosteric mutant-selective fourth-generation EGFR inhibitors as an efficient combination therapeutic in the treatment of non-small cell lung carcinoma.
Sign Up to like & getrecommendations! Published in 2021 at "Drug discovery today"
DOI: 10.1016/j.drudis.2021.02.005
Abstract: Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) are preferred treatments for non-small cell lung carcinoma (NSCLC) that have EGFR activating mutations. Although the initial responses to first- to third-generation EGFR-TKIs is impressive, these agents… read more here.
Keywords: generation egfr; egfr; egfr inhibitors; non small ... See more keywords
Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.08.031
Abstract: A novel series of 4, 6-disubstituted pyrimidines derivatives were designed, synthesized, and evaluated as epidermal growth factor receptor (EGFR) inhibitors for non-small cell lung cancer(NSCLC). 4, 6-disubstituted pyrimidines as core structure was utilized to substitute… read more here.
Keywords: inhibitors non; egfr inhibitors; cell lung; non small ... See more keywords
Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01041
Abstract: Activating mutations in the epidermal growth factor receptor (EGFR) are frequent oncogenic drivers of non-small-cell lung cancer (NSCLC). The most frequent alterations in EGFR are short in-frame deletions in exon 19 (Del19) and the missense… read more here.
Keywords: macrocyclization quinazoline; based egfr; egfr inhibitors; quinazoline ... See more keywords
Development of Furanopyrimidine-Based Orally Active Third-Generation EGFR Inhibitors for the Treatment of Non-Small Cell Lung Cancer
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c01434
Abstract: The development of orally bioavailable, furanopyrimidine-based double-mutant (L858R/T790M) EGFR inhibitors is described. First, selectivity for mutant EGFR was accomplished by replacing the (S)-2-phenylglycinol moiety of 12 with either an ethanol or an alkyl substituent. Then,… read more here.
Keywords: cancer cells; development; egfr inhibitors; furanopyrimidine based ... See more keywords
Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01612
Abstract: Adenosine triphosphate (ATP)-competitive inhibitors of the epidermal growth factor receptor (EGFR) have provided a significant improvement in the disease outcome of nonsmall cell lung cancer (NSCLC). Unfortunately, some marketed drugs affect a transient beneficial response… read more here.
Keywords: anilinoquinazoline scaffold; macrocyclic polyamine; incorporation macrocyclic; egfr inhibitors ... See more keywords
Design, synthesis and biological evaluation of a series of dianilinopyrimidines as EGFR inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2022.2046567
Abstract: Abstract This paper described our efforts to develop dianilinopyrimidines as novel EGFR inhibitors. All the target compounds were tested for inhibitory effects against wild type EGFR (EGFRwt) and three tumour cells, including A549, PC-3, and… read more here.
Keywords: design synthesis; synthesis biological; series dianilinopyrimidines; biological evaluation ... See more keywords
Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2022.2128797
Abstract: Abstract A new series of 5-trifluoromethylpyrimidine derivatives were designed and synthesised as EGFR inhibitors. Three tumour cells A549, MCF-7, PC-3 and EGFR kinase were employed to evaluate their biological activities. The results were shown that… read more here.
Keywords: design synthesis; antitumor activity; egfr inhibitors; synthesis antitumor ... See more keywords