Zhi‐Hao Shi
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View article: Computational-aided understanding of metabolic mechanism: A case study
Computational-aided understanding of metabolic mechanism: A case study Open
This study presents an innovative computational method, combined with experimental validation, to predict and elucidate the metabolic pathways of SILA-123, a novel FLT3 inhibitor. Using UFLC/Q-TOF MS, we identified 21 metabolites generated…
View article: Computational-Aided Understanding of Metabolic Mechanism: A Case Study
Computational-Aided Understanding of Metabolic Mechanism: A Case Study Open
View article: Design, Synthesis, and Biological Evaluation of Flc-8: A Potent Covalent Flt3 Inhibitor for Flt3-Mutant Aml
Design, Synthesis, and Biological Evaluation of Flc-8: A Potent Covalent Flt3 Inhibitor for Flt3-Mutant Aml Open
View article: SP1 undergoes phase separation and activates RGS20 expression through super-enhancers to promote lung adenocarcinoma progression
SP1 undergoes phase separation and activates RGS20 expression through super-enhancers to promote lung adenocarcinoma progression Open
Lung adenocarcinoma (LUAD) is the leading cause of cancer-related death worldwide, but the underlying molecular mechanisms remain largely unclear. The transcription factor (TF) specificity protein 1 (SP1) plays a crucial role in the develo…
View article: Research Progress of Bupleurum Monomer, Drug Therapy and the Treatment of Depression
Research Progress of Bupleurum Monomer, Drug Therapy and the Treatment of Depression Open
Depression has become a very common public health problem worldwide, and its incidence is increasing year by year.At present, antidepressant treatment is mainly based on western medicine, with a single action mechanism, uneven efficacy, st…
View article: Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET Mutations
Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET Mutations Open
Over the past decades, the role of rearranged during transfection (RET) alterations in tumorigenesis has been firmly established. RET kinase inhibition is an essential therapeutic target in patients with RET-altered cancers. In clinical pr…
View article: Insight into Janus kinases specificity: From molecular architecture to cancer therapeutics
Insight into Janus kinases specificity: From molecular architecture to cancer therapeutics Open
Janus Kinases (JAKs) play a crucial role as therapeutic targets for various cancers. However, the current JAK inhibitors (JAKi) available have limited therapeutic benefits due to their lack of selectivity. This review focuses on the struct…
View article: Non-coding RNAs as therapeutic targets in cancer and its clinical application
Non-coding RNAs as therapeutic targets in cancer and its clinical application Open
Cancer genomics has led to the discovery of numerous oncogenes and tumor suppressor genes that play critical roles in cancer development and progression. Oncogenes promote cell growth and proliferation, whereas tumor suppressor genes inhib…
View article: Liver toxicity in rats after subchronic exposure to HTP aerosol and cigarette smoke
Liver toxicity in rats after subchronic exposure to HTP aerosol and cigarette smoke Open
Background Heated tobacco product (HTP) considered to be a novel tobacco product which was reported safer than traditional cigarettes evidenced by lower potential harmful components released. Liver is an important detoxification organ of t…
View article: Preclinical characterization of danatinib as a novel FLT3 inhibitor with excellent efficacy against resistant acute myeloid leukemia
Preclinical characterization of danatinib as a novel FLT3 inhibitor with excellent efficacy against resistant acute myeloid leukemia Open
The therapeutic benefits of available FLT3 inhibitors for AML are limited by drug resistance, which is related to mutations, as well toxicity caused by off-target effects. In this study, we introduce a new small molecule FLT3 inhibitor cal…
View article: Natural products as potential lead compounds to develop new antiviral drugs over the past decade
Natural products as potential lead compounds to develop new antiviral drugs over the past decade Open
View article: Challenges for the development of mutant isocitrate dehydrogenases 1 inhibitors to treat glioma
Challenges for the development of mutant isocitrate dehydrogenases 1 inhibitors to treat glioma Open
View article: Prospects for Anti-Tumor Mechanism and Potential Clinical Application Based on Glutathione Peroxidase 4 Mediated Ferroptosis
Prospects for Anti-Tumor Mechanism and Potential Clinical Application Based on Glutathione Peroxidase 4 Mediated Ferroptosis Open
Ferroptosis, characterized by excessive iron accumulation and lipid peroxidation, is a novel form of iron-dependent cell death, which is morphologically, genetically, and biochemically distinct from other known cell death types, such as ap…
View article: Synthesis and biological evaluation of 4-(4-aminophenyl)-6-methylisoxazolo[3,4-b] pyridin-3-amine covalent inhibitors as potential agents for the treatment of acute myeloid leukemia
Synthesis and biological evaluation of 4-(4-aminophenyl)-6-methylisoxazolo[3,4-b] pyridin-3-amine covalent inhibitors as potential agents for the treatment of acute myeloid leukemia Open
View article: Medicinal Chemistry Strategies for the Development of Bruton’s Tyrosine Kinase Inhibitors against Resistance
Medicinal Chemistry Strategies for the Development of Bruton’s Tyrosine Kinase Inhibitors against Resistance Open
Despite significant efficacy, one of the major limitations of small-molecule Bruton's tyrosine kinase (BTK) agents is the presence of clinically acquired resistance, which remains a major clinical challenge. This Perspective focuses on med…
View article: Gaining Selectivity in the Back Pocket of Fms-Like Tyrosine Kinase 3: A Case Study
Gaining Selectivity in the Back Pocket of Fms-Like Tyrosine Kinase 3: A Case Study Open
View article: Small-Molecule Fms-like Tyrosine Kinase 3 Inhibitors: An Attractive and Efficient Method for the Treatment of Acute Myeloid Leukemia
Small-Molecule Fms-like Tyrosine Kinase 3 Inhibitors: An Attractive and Efficient Method for the Treatment of Acute Myeloid Leukemia Open
Fms-like tyrosine kinase 3 (FLT3) is an important member of the class III receptor tyrosine kinase (RTK) family, which is involved in the proliferation of hematopoietic cells and lymphocytes. In recent years, increasing evidence have demon…
View article: Bio- and medicinally compatible α-amino acid modification via merging photo-redox and N-heterocyclic carbene catalysis
Bio- and medicinally compatible α-amino acid modification via merging photo-redox and N-heterocyclic carbene catalysis Open
An NHC and photo-redox co-catalyzed α-amino acid decarboxylative carbonylation reaction was presented here. This method displayed good scope generality, providing an easy and direct pathway to access various downstream α-amino ketones from…
View article: Bio- and medicinally compatible α-amino acid modification via merging photo-redox and N-heterocyclic carbene catalysis
Bio- and medicinally compatible α-amino acid modification via merging photo-redox and N-heterocyclic carbene catalysis Open
An NHC and photo-redox co-catalyzed α-amino acid decarboxylative carbonylation reaction was presented here. This method displayed good scope generality, providing an easy and direct pathway to access various downstream α-amino ketones from…
View article: Supplementary material to "Sensitivity Analysis of the Surface Ozone and Fine Particulate Matter to Meteorological Parameters in China"
Supplementary material to "Sensitivity Analysis of the Surface Ozone and Fine Particulate Matter to Meteorological Parameters in China" Open
View article: Sensitivity Analysis of the Surface Ozone and Fine Particulate Matter to Meteorological Parameters in China
Sensitivity Analysis of the Surface Ozone and Fine Particulate Matter to Meteorological Parameters in China Open
Meteorological conditions play important roles in the formation of ozone (O3) and fine particulate matter (PM2.5). China has been suffering from serious regional air pollution problems, characterized by high concentrations of surface O3 an…
View article: Total synthesis, chemical modification and structure-activity relationship of bufadienolides
Total synthesis, chemical modification and structure-activity relationship of bufadienolides Open
View article: Recent advance in the development of novel, selective and potent FGFR inhibitors
Recent advance in the development of novel, selective and potent FGFR inhibitors Open
View article: Design, synthesis and evaluation of 2-amino-imidazol-4-one derivatives as potent β-site amyloid precursor protein cleaving enzyme 1 (BACE-1) inhibitors
Design, synthesis and evaluation of 2-amino-imidazol-4-one derivatives as potent β-site amyloid precursor protein cleaving enzyme 1 (BACE-1) inhibitors Open
View article: A novel and efficient synthesis of phenanthrene derivatives via palladium/norbornadiene-catalyzed domino one-pot reaction
A novel and efficient synthesis of phenanthrene derivatives via palladium/norbornadiene-catalyzed domino one-pot reaction Open
Herein we report a novel palladium-catalyzed reaction that results in phenanthrene derivatives using aryl iodides, ortho -bromobenzoyl chlorides and norbornadiene in one pot. This dramatic transformation undergoes ortho- C–H activation, de…
View article: Design, synthesis and structure-activity relationship of diaryl-ureas with novel isoxazol[3,4-b]pyridine-3-amino-structure as multi-target inhibitors against receptor tyrosine kinase
Design, synthesis and structure-activity relationship of diaryl-ureas with novel isoxazol[3,4-b]pyridine-3-amino-structure as multi-target inhibitors against receptor tyrosine kinase Open
View article: Cover Feature: Norbornene‐Mediated Palladium‐Catalysed Domino‐Type Catellani Reaction: an Efficient and Regiospecific Acylation/Suzuki Coupling of Aryl Iodides (Eur. J. Org. Chem. 24/2018)
Cover Feature: Norbornene‐Mediated Palladium‐Catalysed Domino‐Type Catellani Reaction: an Efficient and Regiospecific Acylation/Suzuki Coupling of Aryl Iodides (Eur. J. Org. Chem. 24/2018) Open
The Cover Feature shows the successful application of a palladium-catalysed and norbornene-assisted Catellani reaction towards the synthesis of diaryl ketones. A wide range of aryl iodides with commercially available acyl chlorides as acyl…
View article: CCDC 1837666: Experimental Crystal Structure Determination
CCDC 1837666: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Synthesis and Bioactivity Characterization of Scutellarein Sulfonated Derivative
Synthesis and Bioactivity Characterization of Scutellarein Sulfonated Derivative Open
Scutellarin (1) has been widely used to treat acute cerebral infarction in clinic, but poor aqueous solubility decreases its bioavailability. Interestingly, scutellarin (1) could be metabolized into scutellarein (2) in vivo. In this study,…
View article: Discovery and structure activity relationship of the first potent cryptosporidium FIKK kinase inhibitor
Discovery and structure activity relationship of the first potent cryptosporidium FIKK kinase inhibitor Open