Results 41 to 50 of about 623,955 (160)

The MoSR‐MoDde1 Regulatory Axis: A Novel Determinant of DMI Sensitivity and a Target for Sustainable Rice Blast Control

Advanced Science, EarlyView.
The transcription factor MoSR governs DMI fungicide sensitivity in Magnaporthe oryzae through dual regulation of ergosterol biosynthesis and the detoxification enzyme MoDde1. Targeting MoDde1 via a small‐molecule inhibitor or host‐induced gene silencing enhances DMI efficacy against rice blast, offering a sustainable disease management strategy ...
Fan‐Zhu Meng, Wen‐Kai Wei, Meng‐Yao Wu, Min‐Zheng Cai, Yu‐Fu Wang, Li Zhao, Shuai Meng, Liang‐Fen Yin, Guido Schnabel, Wei‐Xiao Yin, Chao‐Xi Luo   +10 more
wiley   +1 more source

Quinazoline derivatives as anticancer drugs: a patent review (2011-present)

, 2015
International audienceIntroduction: Quinazoline is one of the most studied moieties in medicinal chemistry due to the wide range of biological properties such as the anticancer, antibacterial, anti-inflammatory, antimalarial and antihypertensive ...
Ravez, Severine, Goossens, Laurence, Castillo-Aguilera, Omar, Depreux, Patrick   +3 more
core   +1 more source

A Comprehensive 19F NMR Framework for Fragment‐Based Drug Discovery: The Validated Screening Library OpenFL600 and Efficient Affinity Ranking by CSAR

Angewandte Chemie, Volume 138, Issue 39, 21 September 2026.
NMR screening is a powerful method for hit detection in drug‐discovery. We designed and validated the OpenFL600 19F$^{19}{\rm F}$ NMR library to probe diverse targets, including RNA, GPCRs, kinases, and proteases. This library yields target‐specific ligands without generating promiscuous binders.
Simon H. Rüdisser, Gabriela Stadler, Giacomo Padroni, Daria Barbash, Marco M. Ruckstuhl, Nils Lorz, Christina Jordan, Sarah Skibinski, Timo T. Stühlinger, Sarah E. Kratzwald, Katharina M. Siess, Sven Brüschweiler, Gerald Platzer, Antoine Cléry, Robert Konrat, Frédéric H.‐.T. Allain, Alvar D. Gossert   +16 more
wiley   +2 more sources

One-Pot Synthesis of Isoxazole-Fused Tricyclic Quinazoline Alkaloid Derivatives via Intramolecular Cycloaddition of Propargyl-Substituted Methyl Azaarenes under Metal-Free Conditions

Molecules, 2023
A practical method was developed for the convenient synthesis of isoxazole-fused tricyclic quinazoline alkaloids. This procedure accesses diverse isoxazole-fused tricyclic quinazoline alkaloids and their derivatives via intramolecular cycloaddition of ...
Zhuo Wang, Yuhan Zhao, Jiaxin Chen, Mengyao Chen, Xuehan Li, Ting Jiang, Fang Liu, Xi Yang, Yuanyuan Sun, Yanping Zhu   +9 more
doaj   +1 more source

Novel quinazoline derivatives with biological activity

, 2023
Faculty of Pharmacy in Hradec Králové, Charles University Department of Organic and Bioorganic Chemistry Candidate: Mgr. Zuzana Rania Brožová Supervisor: prof. RNDr. Milan Pour, Ph.D.
Brožová, Zuzana Rania
core  

Comparative Analysis of Molecular Docking Programs GOLD, Glide, and MOE on Quinazoline Derivatives as Antiproliferative Agents: Implications for EGFR-Targeted Therapies

Al-Mustansiriyah Journal of Pharmaceutical Sciences
Background: To aid in the identification of drug candidates and the prediction of protein-ligand interactions, molecular docking predicts how ligands interact with receptors, aiding drug discovery.
Ali Hussein Sabr, Monther Faisal Mahdi, Talal Aburjai   +2 more
doaj   +1 more source

Synthesis of some novel dibromo-2-arylquinazolinone derivatives as cytotoxic agents

Research in Pharmaceutical Sciences, 2019
Recently the quinazoline derivatives have attracted much attention for their anticancer properties. In this study a series of new brominated quinazoline derivatives (1a-1g) were synthesized in two steps.
Zeinab Faghih, Nasrin Rahmannejadi, Razieh Sabet, Kamiar Zomorodian, Mohammad Asad, Soghra Khabnadideh   +5 more
doaj   +1 more source

Low‐Temperature in Situ Upgrading of Ultra‐Deep Heavy Oil Using Ni–Ce/MOF–OTf Superacid Catalysts to Enhance Energy Utilization and Sustainability

EcoEnergy, EarlyView.
A triflate‐functionalized Ni–Ce/MOF–OTf superacid enables low‐temperature (∼140°C) in situ upgrading of ultra‐deep heavy oil. It reduces viscosity by 92.11% in 12 h, maintains activity over cycles, and delivers 90.25% recovery with a lower carbon footprint by selective bond cleavage. ABSTRACT Ultra‐deep heavy oil is an important unconventional resource,
Li Wang, Ji‐Xiang Guo, Qiming Huang, Kunpeng Li, Chi Li, Yajie Wu   +5 more
wiley   +1 more source

The Expanding Role of Diazirines in Synthetic Methodology

European Journal of Organic Chemistry, EarlyView.
Beyond their established role in photoaffinity labeling, diazirines have emerged as versatile reagents in synthetic chemistry. This review highlights their dual reactivity as carbene and nitrogen‐transfer precursors, showcasing mechanistic insights and diverse applications in cyclopropanations, cycloadditions, skeletal editing, amination, heterocycle ...
Viktor Savic, Dominik Schnalzer, Marko D. Mihovilovic, Michael Schnürch   +3 more
wiley   +1 more source

Discovery of Quinazoline-2,4(1H,3H)-Dione Derivatives as Potential Antibacterial Agent: Design, Synthesis, and Their Antibacterial Activity

Molecules, 2022
In this paper, we report on the design and synthesis of a novel series of quinazoline-2,4(1H,3H)-dione derivatives as fluoroquinolone-like inhibitors of bacterial gyrase and DNA topoisomerase IV to identify and develop antimicrobial agents to prevent ...
Nader M. Boshta, Farag A. El-Essawy, Mohammed B. Alshammari, Safaa G. Noreldein, Osama M. Darwesh   +4 more
doaj   +1 more source