A5058045772- Asymmetric Synthesis and Catalysis
- Synthetic Organic Chemistry Methods
- Cancer-related Molecular Pathways
- Catalytic C–H Functionalization Methods
- Asymmetric Hydrogenation and Catalysis
- Synthesis and Catalytic Reactions
- Protein Degradation and Inhibitors
- Advanced Breast Cancer Therapies
- Ubiquitin and proteasome pathways
- Chemical Synthesis and Analysis
- Organoboron and organosilicon chemistry
- Synthesis of Indole Derivatives
- Antibiotic Resistance in Bacteria
- Advanced Synthetic Organic Chemistry
- Bioactive Compounds and Antitumor Agents
- Sulfur-Based Synthesis Techniques
- Chemical synthesis and alkaloids
- Pneumocystis jirovecii pneumonia detection and treatment
- Axial and Atropisomeric Chirality Synthesis
- Organic and Inorganic Chemical Reactions
- Catalytic Alkyne Reactions
- Innovative Microfluidic and Catalytic Techniques Innovation
- Biochemical and Molecular Research
- Organophosphorus compounds synthesis
- Alkaloids: synthesis and pharmacology
Sichuan University
2013-2025
The Wistar Institute
2019-2023
Chengdu University
2014-2021
KTH Royal Institute of Technology
2016
State Key Laboratory of Biotherapy
2009-2014
Army Medical University
2012
Triple-negative breast cancers (TNBC) frequently inactivate p53, increasing their aggressiveness and therapy resistance. We identified an unexpected protein vulnerability in p53-inactivated TNBC designed a new PROteolysis TArgeting Chimera (PROTAC) to target it. Our PROTAC selectively targets MDM2 for proteasome-mediated degradation with high-affinity binding VHL recruitment. loss p53 mutant/deleted cells two-dimensional/three-dimensional culture patient explants, including relapsed tumors,...
Quite a pair: The first organocatalytic direct asymmetric reduction of unprotected 1H-indoles to chiral indolines has been developed. reaction proceeds through the generation electrophilic indolenium ions by Brønsted acid, and then Lewis base (1) mediated enantioselective hydride transfer with HSiCl3. A variety were obtained moderate excellent enantioselectivity. MOM=methoxymethyl. Detailed facts importance specialist readers are published as "Supporting Information". Such documents...
How to fuse heterocycles: The direct enamine–imine isomerization of indoles and subsequent intramolecular imino-ene has been observed under Lewis acid catalysis. This unique reaction occurred for that contain a tethered olefin functionality, led fused indoline heterocycles with excellent diastereocontrol (see scheme). Detailed facts importance specialist readers are published as "Supporting Information". Such documents peer-reviewed, but not copy-edited or typeset. They made available...
The first chemo- and α-regioselective asymmetric Michael addition of γ,γ-disubstituted α,β-unsaturated aldehydes to nitroolefins has been presented in excellent diastereo- enantioselectivities (dr up >99:1, 93−96% ee) via dienamine catalysis. adducts have efficiently converted a number optically pure cyclic frameworks with versatile scaffold diversity.
An asymmetric Diels–Alder reaction of 2-methyl-3-indolylmethanols and α,β-unsaturated aldehydes has been developed that relies on in situ generation active indole-2,3-quinodimethane intermediates under mild acidic conditions uses a secondary chiral amine as iminium activation catalyst. array highly enantioenriched tetrahydrocarbazoles have efficiently produced fair to good yields.
An asymmetric dearomatic Diels–Alder protocol for various heteroarenes, such as benzofuran, benzothiophene, or even furan, has been developed via π-system activation. This method involves in situ generation of formal trienamine species embedding a heteroaromatic moiety, and an array chiral fused frameworks with high molecular complexity skeletal diversity were efficiently constructed good to excellent stereoselectivity by the catalysis cinchona-based primary amine.
Abstract Catalytic asymmetric Friedel–Crafts alkylation is a powerful protocol for constructing chiral C(sp 2 )C(sp 3 ) bond. Most previous examples rely on LUMO activation of the electrophiles using catalysts with subsequent attack by electron‐rich arenes. Presented herein an alternative strategy in which HOMO aromatic π system 2‐furfuryl ketones raised through formation formal trienamine species primary amine. Exclusive regioselective at 5‐position occurred alkylidenemalononitriles, and...
Abstract An asymmetric formal [3+3] cycloaddition process with diversely structured aliphatic ketones and electron‐deficient cyclic 1‐azadienes was developed by cascade enamine–enamine catalysis of a cinchona‐based primary amine. This sequence involved domino Michael addition–Mannich reaction to afford spirocyclic architectures in excellent diastereo‐ enantioselectivity. Importantly, high regioselectivity realized for number unsymmetrical ketone substrates.
Inhibition of histone deacetylase 6 (HDAC6) has emerged as a promising therapeutic strategy for the treatment cancer, chemotherapy-induced peripheral neuropathy, and neurodegenerative disease. The recent X-ray crystal structure determination HDAC6 enables an understanding structural features directing affinity selectivity in active site. Here, we present structures five HDAC6-inhibitor complexes that illuminate key molecular inhibitor linker capping groups facilitate differentiate binding to...
Asymmetric Mannich-type reactions are important organic transformations that provide excellent protocols for the synthesis of optically active nitrogen-containing compounds. This article provides an overview on development thiourea-catalyzed asymmetric Mannich or nitro-Mannich including scope, limitations, and applications different catalytic systems. Keywords: Thiourea, reaction, catalysis, organocatalysis, organocatalytic, chemistry, stereoselective hydrogen-bonding donors, monothiourea,...
Deconjugated linear 3,5-dienones with substantial substitutions were used in β,ε-regioselective Diels–Alder cycloadditions 3-olefinic oxindoles <italic>via</italic> trienamine catalysis of cinchona-based primary amines.
Palladium(0)-catalyzed carbocyclization of 1,7-enynes mediated by (chlorodimethylsilyl)pinacolborane proceeds with 1,8-addition the silicon and boron functions to give functionalized cyclohexane derivatives attached exocyclic olefin. A variety chromane dervatives are accessible this method. In contrast analogous reactions 1,6-enynes, configuration newly formed stereogenic center is controlled a present in substrate.
Abstract While significant progress has been made in Diels–Alder cycloadditions of 2,4‐dienals by the formation trienamine intermediates, we report that further extended tetraenamine species can be generated from 2,4,6‐trienal substrates, which subsequently act as 3,6‐regioselective diene partners asymmetric reaction with 3‐olefinic oxindole dienophiles. An array highly functionalized spirocyclic compounds were produced good stereoselectivity up to 96 % ee and greater than 19:1 d.r., fair...
The dopamine transporter (DAT) serves a pivotal role in controlling (DA)-mediated neurotransmission by clearing DA from synaptic and perisynaptic spaces its action at postsynaptic receptors. Major drugs of abuse such as amphetamine cocaine interact with DAT to mediate their effects enhancing extracellular concentrations. We previously identified novel allosteric site the related human serotonin that lies outside central substrate inhibitor binding pocket. used hybrid structure based (HSB)...
An organocatalytic MBH cascade reaction was developed to construct new 3-(α-acrylic acid) benzoxaboroles, designed mimic ‘anchoring’ pharmacophore features of carbapenems, with the aim helping overcome carbapenemase resistance.
β-Nucleosides are fundamental building blocks of biological systems and used as therapeutic agents for the treatment cancer viral infections. This review summarizes stereoselective synthesis β-nucleosides their analogues.
Metalloenzymes have critical roles in a wide range of biological processes and are directly involved many human diseases; hence, they considered as important targets for therapeutic intervention. The specific characteristics metal ion(s)-containing active sites make exploitation metal-binding pharmacophores (MBPs) to inhibitor development targeting metalloenzymes. This Perspective focuses on boron-containing MBPs, which display unique binding modes with metalloenzyme sites, particularly via...