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   Articles with "quinazoline" as a keyword



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A 1,2,3-Triazole Derivative of Quinazoline Exhibits Antitumor Activity by Tethering RNF168 to SQSTM1/P62.

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recommendations! Published in 2022 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.2c00432

Abstract: Quinazoline and its derivatives have drawn much attention in the development of potential antitumor agents. Here, we synthesized a series of 1,2,3-triazole derivatives of quinazoline at the C6 position and evaluated for their cytotoxic activity… read more here.

Keywords: derivative quinazoline; rnf168; sqstm1 p62; quinazoline ... See more keywords
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Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.

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recommendations! 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
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Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.

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recommendations! Published in 2019 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.9b00390

Abstract: Polypharmacology is a promising paradigm in modern drug discovery. Herein, we have discovered a series of novel PI3K and HDAC dual inhibitors in which the hydroxamic acid moiety as the zinc binding functional group was… read more here.

Keywords: quinazoline; design synthesis; biological evaluation; simultaneously targeting ... See more keywords
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Palladium-Catalyzed Oxidative Cycloaddition of Quinazoline-2,4(1H,3H)-diones and Diarylalkynes via C-H/N-H Activation

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recommendations! Published in 2023 at "Synthesis"

DOI: 10.1055/a-2105-2850

Abstract: The oxidative cycloaddition of 3-subsituted quinazoline-2,4(1H,3H)-diones and alkynes has been developed. The reaction is Pd(II)-catalyzed and successfully occurs in the presence of Ag(I) oxidants. This transformation is assumed to proceed by N-H palladation of the… read more here.

Keywords: oxidative cycloaddition; palladium catalyzed; quinazoline; quinazoline diones ... See more keywords
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Introduction of pyrrolidineoxy or piperidineamino group at the 4-position of quinazoline leading to novel quinazoline-based phosphoinositide 3-kinase delta (PI3Kδ) inhibitors

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recommendations! Published in 2018 at "Journal of Enzyme Inhibition and Medicinal Chemistry"

DOI: 10.1080/14756366.2018.1444608

Abstract: Abstract Phosphoinositide 3-kinase Delta (PI3Kδ) plays a key role in B-cell signal transduction and inhibition of PI3Kδ was confirmed to have clinical benefit in certain types of activation of B-cell malignancies. Herein, we reported a… read more here.

Keywords: quinazoline; kinase delta; pi3k; pyrrolidineoxy piperidineamino ... See more keywords
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Preparation of skeletally diverse quinazoline-2,4(1H,3H)-diones using Na2SiO3/SnFe2O4 catalytic system through a four-component reaction

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recommendations! Published in 2020 at "Main Group Metal Chemistry"

DOI: 10.1515/mgmc-2020-0008

Abstract: Abstract Sodium silicate with the formula of Na2SiO3 was used for the four-component reaction of ketones, aldehydes and cyanoacetamide. The effect of SnFe2O4 nano-particles on the catalytic potential of Na2SiO3 was investigated. The desired products… read more here.

Keywords: quinazoline; component reaction; four component; snfe2o4 ... See more keywords
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Discovery of quinazoline compound as a novel nematicidal scaffold.

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recommendations! Published in 2023 at "Pesticide biochemistry and physiology"

DOI: 10.2139/ssrn.4248671

Abstract: With the aim of discovering novel nematicidal scaffolds, the nematicidal activities of a series of quinazoline compounds were tested, with some compounds showing excellent results. Among them, the LC50 values of compound K11 against Bursaphelenchus… read more here.

Keywords: compound; compound k11; quinazoline; nematicidal scaffold ... See more keywords
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Synthesis, Molecular Docking, biological potentials, and Structure-Activity Relationship of new quinazoline & quinazoline-4-one derivatives.

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recommendations! Published in 2021 at "Current pharmaceutical biotechnology"

DOI: 10.2174/1389201022666210601170650

Abstract: CONTEXT Quinazolines are a common class of nitrogen-containing heterocyclic scaffolds exhibiting a broad spectrum of pharmacological activities. OBJECTIVE In the present study, quinazoline and quinazolin-4-one derivatives were prepared, characterized to evaluate their biological which may… read more here.

Keywords: quinazoline; anti inflammatory; one derivatives; activity ... See more keywords
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Bestowal of Quinazoline Scaffold in Anticancer Drug Discovery.

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recommendations! Published in 2020 at "Anti-cancer agents in medicinal chemistry"

DOI: 10.2174/1871520620666200627205321

Abstract: BACKGROUND Cancer is one of the major causes of worldwide human mortality. A number of existing antineoplastic medications and treatment regimens are already working in the field and several new compounds are in different phases… read more here.

Keywords: quinazoline; chemistry; quinazoline derivatives; quinazoline scaffold ... See more keywords
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Carbonic Anhydrase Inhibition Activities of Schiff’s Bases Based on Quinazoline-Linked Benzenesulfonamide

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recommendations! Published in 2022 at "Molecules"

DOI: 10.3390/molecules27227703

Abstract: Human carbonic anhydrase (CA, EC 4.2.1.1) (hCA) isoforms I, II, IX, and XII were investigated for their inhibitory activity with a series of new Schiff’s bases based on quinazoline scaffold 4–27. The hCA I isoform… read more here.

Keywords: schiff bases; carbonic anhydrase; quinazoline; hca inhibitors ... See more keywords
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A Review on the Synthesis and Chemical Transformation of Quinazoline 3-Oxides

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recommendations! Published in 2022 at "Molecules"

DOI: 10.3390/molecules27227985

Abstract: The synthesis of quinazoline 3-oxides and their derivatives has attracted considerable attention due to their reactivity as intermediates in the synthesis of quinazoline analogues and their ring-expanded derivatives. Despite this, there is no comprehensive review… read more here.

Keywords: chemical transformation; quinazoline; quinazoline oxides; synthesis chemical ... See more keywords