A New Route for the Synthesis of (Trichloromethyl)Quinazoline‐4(1H)‐One and (1,2,3‐Triazole)‐Quinazoline‐4(1H)‐One Functionalized Derivatives via Copper‐Catalyzed One‐Pot Multicomponent Reactions
Sign Up to like & getrecommendations! Published in 2024 at "Journal of Heterocyclic Chemistry"
DOI: 10.1002/jhet.4899
Abstract: The synthesis of functionalized (trichloromethyl)quinazoline‐4(1H)‐one with high yields through a novel three‐component intramolecular CH activation reaction from trichloroacetonitrile, benzoyl chlorides, and various primary amines is a remarkable achievement in organic chemistry. This strategy offers a… read more here.
Keywords: chemistry; quinazoline; triazole quinazoline; synthesis ... See more keywords
New Tricyclic Aryl Quinazoline Derivatives by Suzuki‐Miyaura Cross‐Coupling
Sign Up to like & getrecommendations! Published in 2024 at "ChemistryOpen"
DOI: 10.1002/open.202400197
Abstract: Abstract A number of new deoxyvasicinone (2,3‐dihydropyrrolo[2,1‐b]quinazolin‐9(1H)‐one) and mackinazolinone (6,7,8,9‐tetrahydro‐11H‐pyrido[2,1‐b]quinazolin‐11‐one) derivatives with aryl substituents at C7/C8 and at C5 are reported. These compounds are rare representatives of their kind and were prepared in high yields… read more here.
Keywords: suzuki miyaura; cross coupling; miyaura cross; aryl ... See more keywords
A 1,2,3-Triazole Derivative of Quinazoline Exhibits Antitumor Activity by Tethering RNF168 to SQSTM1/P62.
Sign Up to like & getrecommendations! 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
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
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
Sign Up to like & getrecommendations! 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
Identification of Novel Quinolone and Quinazoline Alkaloids as Phosphodiesterase 10A Inhibitors for Parkinson’s Disease through a Computational Approach
Sign Up to like & getrecommendations! Published in 2024 at "ACS Omega"
DOI: 10.1021/acsomega.3c10351
Abstract: Phosphodiesterases (PDEs) are vital in signal transduction, specifically by hydrolyzing cAMP and cGMP. Within the PDE family, PDE10A is notable for its prominence in the striatum and its regulatory function over neurotransmitters in medium-spiny neurons.… read more here.
Keywords: cns active; quinazoline; pde10a; quinolone ... See more keywords
Palladium-Catalyzed Oxidative Cycloaddition of Quinazoline-2,4(1H,3H)-diones and Diarylalkynes via C-H/N-H Activation
Sign Up to like & getrecommendations! 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
Introduction of pyrrolidineoxy or piperidineamino group at the 4-position of quinazoline leading to novel quinazoline-based phosphoinositide 3-kinase delta (PI3Kδ) inhibitors
Sign Up to like & getrecommendations! 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
Preparation of skeletally diverse quinazoline-2,4(1H,3H)-diones using Na2SiO3/SnFe2O4 catalytic system through a four-component reaction
Sign Up to like & getrecommendations! 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
Discovery of quinazoline compound as a novel nematicidal scaffold.
Sign Up to like & getrecommendations! 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
Synthesis, Molecular Docking, biological potentials, and Structure-Activity Relationship of new quinazoline & quinazoline-4-one derivatives.
Sign Up to like & getrecommendations! 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