Design and synthesis of novel quinazolin‐4(1H)‐one derivatives as potent and selective inhibitors targeting AKR1B1
Sign Up to like & getrecommendations! Published in 2023 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200577
Abstract: Inhibition of aldose reductase (AKR1B1) is a promising option for the treatment of diabetic complications. However, most of the developed small molecule inhibitors lack selectivity or suffer from low bioactivity. To address this limitation, a… read more here.
Keywords: design synthesis; derivatives potent; quinazolin one; selective inhibitors ... See more keywords
Novel spiro[indene‐1,2′‐quinazolin]‐4′(3′H)‐one derivatives as potent anticonvulsant agents: One‐pot synthesis, in vivo biological evaluation, and molecular docking studies
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Biochemical and Molecular Toxicology"
DOI: 10.1002/jbt.23234
Abstract: A new series of spiro[indene‐1,2′‐quinazolin]‐4′(3′H)‐one derivatives 4a–m were synthesized via a one‐pot method and evaluated for anticonvulsant activities using pentylenetetrazole (PTZ) and maximal electroshock (MES)‐induced seizures. Obtained results demonstrated that these compounds have not anticonvulsant… read more here.
Keywords: spiro indene; compound; quinazolin one; indene quinazolin ... See more keywords
Quinazolin-4(3H)-one based agents bearing thiadiazole-urea: Synthesis and evaluation of anti-proliferative and antiangiogenic activity.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.104553
Abstract: A series of quinazolin-4(3H)-one based agents containing thiadiazole-urea were designed, synthesized, and biologically evaluated. The proliferation rate of PC3 cells was moderately reduced by compound 9f (IC50 = 17.7 μM)which was comparable with sorafenib (IC50 = 17.3 μM). There… read more here.
Keywords: agents bearing; based agents; one based; quinazolin one ... See more keywords
11H-Pyrido[2,1-b]quinazolin-11-one - A reversible Turn-on/off Fluorescent Probe for Solution and Gas-phase Detection of Acids or Basic Amines
Sign Up to like & getrecommendations! Published in 2021 at "Dyes and Pigments"
DOI: 10.1016/j.dyepig.2021.109536
Abstract: Abstract The present study details a metal- and solvent-free synthesis of 11H-pyrido[2,1-b]quinazolin-11-one (1) and its photophysical properties as an acid or base-sensitive sensor. The absorption spectra in organic solvents revealed a small blue shift on… read more here.
Keywords: basic amines; quinazolin one; pyrido quinazolin; acids basic ... See more keywords
Synthesis and evaluation of new quinazolin-4(3H)-one derivatives as potent antibacterial agents against multidrug resistant Staphylococcus aureus and Mycobacterium tuberculosis.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.04.067
Abstract: Staphylococcus aureus and Mycobacterium tuberculosis are major causative agents responsible for serious nosocomial and community-acquired infections impacting healthcare systems globally. Over several decades, these pathogens have developed resistance to multiple antibiotics significantly affecting morbidity and… read more here.
Keywords: antibacterial agents; one derivatives; quinazolin one; staphylococcus aureus ... See more keywords
Discovery of 2-(Pyrazol-4-yl)-quinazolin-4(3H)-one Derivatives as Subnanomolar BRD4 BD2 Inhibitors with High Selectivity via a Bioisosterism Approach.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c00924
Abstract: BRD4, a bromodomain-containing protein, has emerged as an attractive therapeutic target for various diseases. Selective inhibition of the bromodomain is gaining traction as a promising strategy for targeted drug discovery. Based on bioisosterism-guided optimization of… read more here.
Keywords: brd4 bd2; one derivatives; pyrazol quinazolin; quinazolin one ... See more keywords
Synthesis and Antitumor Activity of 6-(2-Aminobenzo[d]thiazol-5-yl) quinazolin-4(3H)-one Derivatives
Sign Up to like & getrecommendations! Published in 2025 at "ACS Omega"
DOI: 10.1021/acsomega.4c08645
Abstract: Quinazolinones are key scaffolds in anticancer drug development. We previously identified the lead compound 16h from a series of 6-(1H-benzo[d]imidazol-6-yl) quinazolin-4(3H)-one derivatives. In this study, we optimized 16h to develop new 6-(2-aminobenzo[d]thiazol-5-yl) quinazolin-4(3H)-one derivatives, with… read more here.
Keywords: aminobenzo thiazol; quinazolin one; one derivatives; thiazol quinazolin ... See more keywords
Quinazolin-4(3H)-one based potential multiple tyrosine kinase inhibitors with excellent cytotoxicity
Sign Up to like & getrecommendations! Published in 2021 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2021.1972992
Abstract: A series of quinazolin-4(3H)-one derivatives were synthesised and evaluated for their cytotoxicity against human Caucasian breast adenocarcinoma (MCF-7) and human ovarian carcinoma (A2780) cell lines. Cytotoxicity of the most tested compounds was 2- to 30-fold… read more here.
Keywords: multiple tyrosine; one derivatives; kinase; quinazolin one ... See more keywords
Synthesis and corrosion inhibition effects of quinazolin-(3H)-4-one derivatives containing long-chain pyridinium salts on carbon steel in 1.5 M HCl
Sign Up to like & getrecommendations! Published in 2017 at "Protection of Metals and Physical Chemistry of Surfaces"
DOI: 10.1134/s2070205117050161
Abstract: Quinazolin-4(3H)-one derivatives containing long-chain pyridinium salts were synthesized by a quaternization reaction of pyridine. The confirmation of the synthesized compounds structure was performed by FT-IR, 1H NMR and 13C NMR spectroscopy. Corrosion inhibition tests were… read more here.
Keywords: chain; corrosion inhibition; inhibition; corrosion ... See more keywords
Synthesis and Anti-Proliferative Evaluations of New Heterocyclic Derivatives using 5,6,8,9-tetrahydropyrazolo[5,1-b]quinazolin-7(3H)-one Derivatives Derived from Cyclohexa-1,4-dione.
Sign Up to like & getrecommendations! Published in 2020 at "Anti-cancer agents in medicinal chemistry"
DOI: 10.2174/1871520620666200523162549
Abstract: BACKGROUND Recentlty pyrazoloquinazoline derivatives acquired a special attention due to their wide range of pharmacological activities especially the therapeutic activities. Through the market it was found that many pharmacological drugs containing the quinazoline nucleus were… read more here.
Keywords: tetrahydropyrazolo quinazolin; one derivatives; derivatives using; quinazolin one ... See more keywords
Computational design of quinazolin-4(3H)-one derivatives as multitarget inhibitors against angiogenesis and metabolic reprogramming to help overcome cancer resistance
Sign Up to like & getrecommendations! Published in 2025 at "Arabian Journal of Chemistry"
DOI: 10.25259/ajc_159_2024
Abstract: Dysfunction of receptor tyrosine kinases (RTKs) in angiogenesis significantly contributes to cancer progression. However, inhibiting primary angiogenesis pathways often leads to acquired resistance through various mechanisms, including alternative pathways. Targeting both angiogenesis and tumor energy… read more here.
Keywords: cancer; resistance; computational design; quinazolin one ... See more keywords