A5001926861- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Asymmetric Synthesis and Catalysis
- Synthetic Organic Chemistry Methods
- Catalytic C–H Functionalization Methods
- Axial and Atropisomeric Chirality Synthesis
- Asymmetric Hydrogenation and Catalysis
- Chemical synthesis and alkaloids
- Synthesis and biological activity
- PI3K/AKT/mTOR signaling in cancer
- Oxidative Organic Chemistry Reactions
- Molecular spectroscopy and chirality
- Synthesis of Organic Compounds
- Polyamine Metabolism and Applications
- Cancer therapeutics and mechanisms
- Multicomponent Synthesis of Heterocycles
- Supramolecular Self-Assembly in Materials
- Ginkgo biloba and Cashew Applications
- Photoreceptor and optogenetics research
- Metabolism and Genetic Disorders
- Synthesis and pharmacology of benzodiazepine derivatives
- Cancer Treatment and Pharmacology
- Folate and B Vitamins Research
- Chemical Synthesis and Analysis
- Catalytic Cross-Coupling Reactions
Chinese University of Hong Kong
2022-2024
Central South University
2015-2022
Sun Yat-sen University
2018-2021
National Institute of Clean and Low-Carbon Energy
2018-2019
The first iridium-catalyzed enantioselective intramolecular allylic aminations of benzimidazole-tethered carbonates were developed, providing three classes tricyclic benzimidazoles bearing a tertiary carbon stereogenic center in high yields and excellent enantioselectivities (up to 99% yield, ee). Wide substrate scope, catalytic efficiency mild conditions rendered this protocol particularly superior practical. Impressively, the chiral bridge with tunable structure was shown provide very good...
A series of chiral heterocyclic biaryls with a pyridyl moiety were prepared in moderate to good yields up 92% ee <italic>via</italic> asymmetric Suzuki–Miyaura coupling.
Precise transformations of natural products (NPs) can fine-tune their physicochemical properties while preserving inherently complex and evolutionarily optimized parent scaffolds. Here, we report an unprecedented lactone-to-lactam transformation on bilobalide, thus improving its stability paving the way for biological exploration previously inaccessible chemical space that is highly representative structure. This late-stage molecular editing bilobalide enables facile access to a unique...
Twenty-eight novel 1,5-disubstituted-2(1H)-pyridone derivatives were designed and synthesized for discovering more potent anti-lung cancer agents combined with anti-fibrotic profiles. The in vitro antiproliferative activities of the against A549 NIH3T3 cell lines tested by MTT assays. majority analogues exhibited equivalent or an improved activity. Prominently, compound 4l displayed best potency selectivity toward IC50 value 20 μM, nearly comparable to positive control cisplatin (IC50 = 10...
As an important regulator of cell metabolism, proliferation, and survival, mTOR (mammalian target rapamycin) signaling provides both a potential for cancer treatment research tool investigation metabolism. One inhibitor mTORC1 mTORC2 pathways, OSI-027, exhibited robust anticancer efficacy but induced side effects. Herein, we designed photoactivatable OSI-027 prodrug, which allowed the release after light irradiation to inhibit pathway, triggering autophagy leading death. This prodrug can...
A Brønsted acid‐catalyzed aza‐Mannich reaction between 3‐hydroxyisoindolin‐1‐ones and N ‐ tert ‐butyl hydrazones was developed. Under the catalysis of racemic phosphoric acid or trifluoroacetic mild conditions, this domino allows for efficient synthesis 3‐(hydrazono)isoindolin‐1‐one derivatives in excellent yields with high chemoselectivities. The E ‐configuration hydrazone products determined by X‐ray single‐crystal diffraction 5w .
By means of the direct condensation N-aminoethylpyrroles and isatins, followed by a chiral phosphoric acid-catalyzed asymmetric intramolecular Friedel-Crafts reaction, new class valuable 3',4'-dihydro-2'H-spiro[indoline-3,1'-pyrrolo[1,2-a]pyrazin]-2-ones bearing quaternary carbon stereocenter were successfully synthesized in good to excellent yields with moderate enantioselectivities under mild reaction conditions.
Abstract The iridium‐catalysed enantioselective intramolecular allylic substitution of pyrimidine‐tethered carbonates was developed. A wide range chiral pyrimidine‐fused diazepinone derivatives were successfully constructed in 88–96% yields with 85–99% ees. This work further highlights the power chiral‐bridged biphenyl phosphoramidites asymmetric synthesis. magnified image
Abstract Using dppe as the ligand, Nickel‐catalyzed decarbonylative cycloaddition of benzofuran‐2,3‐diones with alkynes was established, and a variety functional flavones were synthesized in 65–99% yields. Terminal substituted phenyl groups internal such aryl acyl acetylenes diphenylacetylenes are suitable for this reaction. The effects bases on reactions different types alkyne substrates also investigated discussed. magnified image
Abstract A class of chiral sulfinamide monophosphine ligands Ming‐Phos were firstly employed in the asymmetric Suzuki coupling reactions. Using in‐situ formed catalyst from PdCl 2 and ( R, S )‐ M07 , 22 axially phosphonates or phosphine oxides successfully synthesized 29−99% yields with up to 98% ee. This method provides a simple efficient protocol for synthesis biaryl oxides.
A series of novel pyrazolo[3,4-b]pyridine derivatives were designed, synthesized, and biologically evaluated for anti-lung cancer activity. Structure-activity relationship AutoGPA models constructed based on the in vitro antiproliferative potency compounds against a human lung adenocarcinoma cell line (A549). Compound 9d exhibits improved A549 growth inhibition (3.06 ± 0.05 μM) compared with A-769662 (45.29 2.14 μM). can elevate phosphorylation levels adenosine monophosphate-activated...