A5060049267- Synthetic Organic Chemistry Methods
- Asymmetric Synthesis and Catalysis
- Synthesis and biological activity
- Asymmetric Hydrogenation and Catalysis
- Quinazolinone synthesis and applications
- Chemical Synthesis and Analysis
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Catalytic Alkyne Reactions
- Click Chemistry and Applications
- Catalytic C–H Functionalization Methods
- Synthesis and Characterization of Heterocyclic Compounds
- Cancer therapeutics and mechanisms
- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- Catalytic Cross-Coupling Reactions
- Synthesis and Biological Evaluation
- Cyclopropane Reaction Mechanisms
- Synthesis and Catalytic Reactions
- Lung Cancer Treatments and Mutations
- Oxidative Organic Chemistry Reactions
- Microbial Natural Products and Biosynthesis
- Cytokine Signaling Pathways and Interactions
- Cancer Mechanisms and Therapy
- Biochemical and Molecular Research
- Advanced Synthetic Organic Chemistry
Mansoura University
2016-2025
Al Wataniya Private University
2022
Aswan University
2020
Korea Institute of Science and Technology
2012-2019
Institut des Molécules et Matériaux du Mans
2014
Université Nantes Angers Le Mans
2012-2014
Le Mans Université
2012-2014
Centre National de la Recherche Scientifique
2012-2014
Kyoto University
2007-2012
Gamma rules: The title reaction was achieved in a highly regioselective manner using aryl Grignard reagents with monodentate chiral N-heterocyclic carbene–copper(I) catalyst to give diarylvinylmethanes excellent enantiomeric excess yield (see scheme). Detailed facts of importance specialist readers are published as "Supporting Information". Such documents peer-reviewed, but not copy-edited or typeset. They made available submitted by the authors. Please note: publisher is responsible for...
We report the synthesis of new series 1,3,5-triazines and 2-phenylquinazolines as anti-cancer agents. Compounds 4a-c, 5c, 5g, 5m showed highest cytotoxic effect against, most notably, leukemia, non-small cell lung cancer, colon carcinoma, CNS melanoma renal cancer. The inhibitory activity against three different kinases; PI3K-α, B-Raf VEGFR-2, was tested for active candidates. compounds exhibited notable PI3K-α inhibitors where compound 5g found to have effect, 4c 5c good activities 4b had...
Chiral N-heterocyclic carbene ligands were electronically and sterically tuned to improve γ-selectivity in copper(I)-catalyzed asymmetric allylic arylation of aliphatic bromides with several aryl Grignard reagents. High was realized when either the group reagent or on N-substituent ligand electron-deficient bromide bulky. The results indicated that electron deficiency steric hindrance initially formed σ-allyl copper intermediate enhance rate reductive elimination give γ-products as major isomers.
Phenyl- and ethyl-magnesium bromides undergo regioselective asymmetric allylic substitution with high enantioselectivity under the catalysis of chiral amidophosphane–copper(I) complexes.
Gamma ist entscheidend: Die Titelreaktion gelang hoch regioselektiv mit Aryl-Grignard-Reagentien und einem Kupfer(I)-Katalysator einzähnigem chiralem N-heterocyclischem Carbenliganden lieferte Diarylvinylmethane ausgezeichnetem Enantiomerenüberschuss in hoher Ausbeute (siehe Schema).
A catalytic 1,3-dipolar cycloaddition between carboalkoxy ketonitrones and methacrolein under the effect of chiral ruthenium Lewis acid (R,R-1) was developed with high regio-, diastereo-, enantiocontrol. The diastereochemical outcome reaction is marked by a significant solvent effect, divergent endo or exo control can be tuned an appropriate choice both N- O-substituents ketonitrone. rationale based on computational study interactions methacrolein-Ru complex its counteranion (SbF6(-)),...
To develop multitarget-directed ligands (MTDLs) as potential treatments for Alzheimer's disease (AD) and to shed light on the effect of chromene group in designing these ligands, 35 new tacrine-chromene derivatives were designed, synthesized, biologically evaluated. Compounds 5c 5d exhibited most desirable multiple functions AD; they strong hAChE inhibitors with IC50 values 0.44 0.25 μM, respectively. Besides, their potent BuChE inhibitory activity was 10- 5-fold more active than...
ABSTRACT Novel thienopyrimidinone hybrids 5–25 were developed and synthesized as potential inhibitors of human EGFR FGFR. The in vitro antiproliferative action all compounds, towards the breast tumor cells MDA‐MB‐231 MCF‐7, was evaluated with doxorubicin serving a reference (IC 50 = 6.72 µM). Compound 23 demonstrated highest anti‐breast cancer efficacy against both cellular lines having IC ranging from 2.95 to 3.80 µM. enzyme inhibition FGFR by most active candidates 18 , 21 23–25 further...
Abstract Peptidic modification of ( S )‐2‐[(diphenylphosphino)methyl]pyrrolidine gave a dipeptide‐connected amidomonophosphane ligand for the highly efficient, copper‐catalyzed asymmetric conjugate addition reaction organozinc reagents with cycloalkenones, giving 3‐alkylated cycloalkanones in high enantioselectivity up to 98 % ee . A model that predicts stereochemistry is discussed.
Anaplastic lymphoma kinase (ALK) has been recognised as a promising molecular target of targeted therapy for NSCLC. We performed SAR study pyrazolo[3,4-b]pyridines to override crizotinib resistance caused by ALK-L1196M mutation and identified novel potent L1196M inhibitor, 10g. 10g displayed exceptional enzymatic activities (<0.5 nM IC50) against well ALK-wt. In addition, is an extremely inhibitor ROS1 displays excellent selectivity over c-Met. Moreover, strongly suppresses proliferation...
The asymmetric conjugate addition of dialkylzinc reagents to racemic 6-substituted cyclohexenones under the catalysis chiral amidophosphane-copper(I) complexes gave a mixture nearly equal amounts corresponding trans- and cis-disubstituted cyclohexanones with extremely high catalyst-controlled enantioselectivity. Epimerization 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) led conversion these mixtures into thermodynamically more stable trans-2,5-disubstituted cyclohexanone as major product up 96%...