A5101438112- Fibroblast Growth Factor Research
- Liver physiology and pathology
- Kruppel-like factors research
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- PI3K/AKT/mTOR signaling in cancer
- Cancer, Hypoxia, and Metabolism
- Cancer Mechanisms and Therapy
- Lung Cancer Treatments and Mutations
- Cancer therapeutics and mechanisms
- Phagocytosis and Immune Regulation
- Pancreatic and Hepatic Oncology Research
- Eosinophilic Disorders and Syndromes
- Protein Kinase Regulation and GTPase Signaling
- Metal-Organic Frameworks: Synthesis and Applications
- Epigenetics and DNA Methylation
- Drug Transport and Resistance Mechanisms
- Cytokine Signaling Pathways and Interactions
- Cancer-related gene regulation
- Covalent Organic Framework Applications
- Mast cells and histamine
- Quinazolinone synthesis and applications
- Angiogenesis and VEGF in Cancer
- Microbial Natural Products and Biosynthesis
- Hepatocellular Carcinoma Treatment and Prognosis
Chinese Academy of Sciences
2016-2025
University of Chinese Academy of Sciences
2016-2025
Shanghai Institute of Materia Medica
2016-2025
Chinese Center For Disease Control and Prevention
2025
State Key Laboratory of Drug Research
2015-2025
Advanced Research Institute
2025
North China University of Science and Technology
2024
Levine Cancer Institute
2020-2024
Hebei General Hospital
2024
Xiangya Hospital Central South University
2023
Abstract Ultrafine gold nanoclusters (Au‐NCs) are susceptible to migrate and aggregate, even in the porosity of many crystalline solids. N‐heterocyclic carbenes (NHCs) a class structurally diverse ligands for stabilization Au‐NCs homogeneous chemistry, showing catalytic reactivity CO 2 activation. Herein, first time, we demonstrate heterogeneous nucleation approach stabilize ultrasmall highly dispersed an NHC‐functionalized porous matrix. The sizes tunable from 1.3 nm 1.8 based on...
A microporous Cu-MOF with optimized open metal sites and pore space was constructed based on a designed bent ligand; it exhibits high-capacity multiple gas storage under atmospheric pressure efficient catalytic activity for chemical fixation of CO2 mild conditions.
Abstract One of the biggest hurdles for development metabolism-targeted therapies is to identify responsive tumor subsets. However, metabolic vulnerabilities most human cancers remain unclear. Establishing link between signatures and oncogenic alterations receptor tyrosine kinases (RTK), well-defined cancer genotypes, may precisely direct intervention a broad patient population. By integrating metabolomics transcriptomics, we herein show that RTK activation causes distinct preference....
By use of an improved synthetic strategy, a series 3,5-disubstituted and 3,5,7-trisubstituted quinolines were readily prepared. 3,5,7-Trisubstituted 21a-c, 21l, 27a-c identified as the most potent c-Met inhibitors with IC(50) less than 1.0 nM. Compound 21b showed promising overall PK profile has high potency extraordinary selectivity to against family member Ron 12 other tyrosine kinases. It produced constitutive inhibition phosphorylation in dependent cell lines. At doses 100 mg/kg,...
A zirconium-phosphonate network, as a bifunctional catalyst for carbon dioxide (CO2)/epoxide coupling reaction, exhibits very high activity that is superior to most documented metal-organic framework (MOF)-based catalysts. Furthermore, it possesses extraordinary tolerance extremely harsh conditions, such aqua regia. This paper describes the use of metal phosphonate new MOF applied CO2 transformation.
Exploitation of new materials for the removal long-lived and highly radioactive actinides their fission products produced in nuclear fuel cycle is crucial radionuclide management. Here, two rare porous anionic uranyl-organic frameworks (UOFs) have been successfully synthesized by a judicious combination tetratopic carboxylate ligand 1,3,6,8-tetrakis( p-benzoic acid)pyrene (H4TBAPy) D3 h-symmetrical triangular [UO2(COO)3]-. The resulting compounds exhibit different architectures, albeit with...
Fibroblast growth factor receptors (FGFRs) are important targets for cancer therapy. Herein, we describe the design, synthesis, and biological evaluation of a novel series 1H-pyrazolo[3,4-b]pyridine derivatives as potent selective FGFR kinase inhibitors. On basis its excellent in vitro potency favorable pharmacokinetic properties, compound 7n was selected vivo showed significant antitumor activity FGFR1-driven H1581 xenograft model. These results indicated that would be promising candidate...
Blockade of immune checkpoint PD-1/PD-L1 has been a promising anticancer strategy; however, clinically available small-molecule inhibitors are lacking. In view the high potency compound 2 (BMS-1002), structural fine tuning methoxy linkage together with diverse modification in solvent interaction region was conducted. A series novel derivatives featuring difluoromethyleneoxy were designed. Compound 43 identified as most inhibitor an IC50 value 10.2 nM HTRF assay. This is capable promoting...
Expression of the polymeric immunoglobulin receptor (pIgR), a transporter IgA and IgM, is commonly increased in response to viral or bacterial infections, linking innate adaptive immunity. Abnormal expression pIgR cancer was also observed, but its clinical relevance remains uncertain. A human hepatocellular carcinoma (HCC) tissue microarray (n = 254) used investigate association between early recurrence. An experimental lung metastasis model using severe combined immune-deficient mice...
Effusin A (1), a spirobicyclic N,O-acetal derivative with an unprecedented 3′,3a′,5′,6′-tetrahydrospiro[piperazine-2,2′-pyrano[2,3,4-de]chromene] ring system, and spiro-polyketide-diketopiperazine hybrid dihydrocryptoechinulin D (2) were isolated from mangrove rhizosphere soil derived fungus, Aspergillus effuses H1-1. Their structures determined by detailed spectroscopic analysis. (1) occurred as racemates, the enantiomers of which separated characterized online HPLC-ECD analysis their...
Seven new prenylated indole diketopiperazines, versicamides A–G (1–7) and a novel chemical derivative from 7, versicamide H (8), along with three known analogic diketopiperazines (9–11) were obtained the marine-derived fungus Aspergillus versicolor HDN08-60. Their structures determined by spectroscopic techniques, including 2D NMR, ECD calculations, single-crystal X-ray diffraction analysis, together assistance of further conversions. The cytotoxicities 1–8 tested against HeLa, HCT-116,...
Deregulation of the immune system is believed to contribute cancer malignancy, which has led recent therapeutic breakthroughs facilitating antitumor immunity. In a malignant setting, immunoglobulin receptors, are fundamental components human system, fulfill paradoxical roles in pathogenesis. This study describes previously unrecognized pro‐oncogenic function polymeric receptor (pIgR) promotion cell transformation and proliferation. Mechanistically, pIgR overexpression associated with YES...
A novel 3D copper-phosphonate network, with the general formula Cu7(H1L)2(TPT)3(H2O)6, namely compound 1, has been synthesized using a rigid tetrahedral linker tetraphenylsilane tetrakis-4-phosphonic acid (H8L) and nitrogen-containing ancillary ligand (TPT: [5-(4-(1H-1,2,4-triazol-1-yl)phenyl)-1H-tetrazole]) under hydrothermal conditions. The was fully characterized PXRD, ICP, IR, TGA elemental analysis. Compound 1 can be used as an efficient catalyst for CO2 coupling reaction that is...
Fibroblast growth factor receptor (FGFR) represents an attractive oncology target for cancer therapy in view of its critical role promoting formation and progression, as well causing resistance to approved therapies. In this article, we describe the identification potent pan-FGFR inhibitor (R)-21c (FGFR1–4 IC50 values 0.9, 2.0, 6.1 nM, respectively). Compound exhibited excellent vitro inhibitory activity against a panel FGFR-amplified cell lines. Western blot analysis demonstrated that...
Laeviganoids A–T (1–20), 20 new ent-clerodane-type diterpenoids featuring a 2-furanone (1–3) or furan (4–20) ring, as well six analogues (21–26), were isolated from the roots of Croton laevigatus. Their structures determined by spectroscopic data analysis, experimental electronic circular dichroism measurements, and X-ray crystallographic studies. Compounds 4–6, 16, 21–24, 26 could influence anti-inflammatory protumoral phenotype macrophages. Among these compounds, 21 are most potent,...
Three highly oxygenated new diterpenes, trigochinins A−C (1−3) were isolated from Trigonostemon chinensis. Their structures with the absolute configuration determined by a spectroscopic method, X-ray crystallography, and CD analysis. This study suggested revision of C-6 stereochemistry trigonothyrins reported quite recently. Compound 3 showed significant inhibition against MET tyrosine kinase activity IC50 value 1.95 μM.
Eucalyptin A (1), together with two known compounds 2 and 3 exhibiting potent inhibition on HGF/c-Met axis, was discovered from the fruits of Eucalyptus globulus. 1 possessed an unprecedented carbon framework phloroglucinol-coupled sesquiterpenoid, its structure elucidated by spectroscopic method ECD calculation. brief structure-activity relationship discussion indicated that coupling a phloroglucinol sesquiterpenoid is essential for activity.
We have developed a series of new 2,4-diarylaminopyrimidine analogues (DAAPalogues) bearing flexible amino acid side chain, different from the majority literature reported ALK inhibitors that often possess structurally constrained arylpiperazine fragment or its equivalents in solvent-interaction region. Extensive structural elaboration led to compound 15 possessing IC50 values 2.7 and 15.3 nM, respectively, wild-type gate-keeper mutant L1196M enzymatic assays. This not only showed high...
c-Met has emerged as an attractive target for targeted cancer therapy because of its abnormal activation in many cells. To identify high potent and selective inhibitors, we started with profiling the potency vitro metabolic stability a reported hit 7. By rational design, novel sulfonylpyrazolo[4,3-b]pyridine 9 improved DMPK properties was discovered. Further elaboration π–π stacking interactions solvent accessible polar moieties led to series highly type I inhibitors. On basis vivo...
A highly stable microporous Mn<sup>II</sup> phosphonate is rationally designed and it exhibits efficient performance in the context of CO<sub>2</sub> chemical conversion into cyclic carbonates under ambient conditions.
Fibroblast growth factor receptor (FGFR) is a potential target for cancer therapy.
c-Met inhibitor JNJ38877605 has proven curative as an antitumor agent, while its clinical study was terminated due to renal toxicity. It reported that the toxicity caused by poor solubility of aldehyde oxidase (AO) metabolites. Therefore, blocking AO oxidation might diminish toxic metabolites and overcome Compound 3, metabolic site deuterated JNJ38877605, then synthesized target molecule. In vitro monkey liver S9 fraction incubation 3 manifested metabolite M2-2 significantly reduced, which...