A5006998500- HIV/AIDS drug development and treatment
- Hepatitis C virus research
- Cancer, Hypoxia, and Metabolism
- Cancer-related Molecular Pathways
- Cancer therapeutics and mechanisms
- Lung Cancer Treatments and Mutations
- Drug Solubulity and Delivery Systems
- Advanced Breast Cancer Therapies
- Biochemical and Molecular Research
- ATP Synthase and ATPases Research
- Tuberculosis Research and Epidemiology
- HER2/EGFR in Cancer Research
- Trypanosoma species research and implications
- Antibiotic Resistance in Bacteria
- Asymmetric Synthesis and Catalysis
- Mitochondrial Function and Pathology
- Crystallization and Solubility Studies
- Protein Kinase Regulation and GTPase Signaling
- Estrogen and related hormone effects
- Organoboron and organosilicon chemistry
- Click Chemistry and Applications
- Chemical Synthesis and Analysis
- Cardiac Ischemia and Reperfusion
- Synthesis and Reactivity of Heterocycles
- Colorectal Cancer Treatments and Studies
Qilu Hospital of Shandong University
2024-2025
Zhejiang University
2025
WuXi AppTec (China)
2014-2024
University of Southern California
2023-2024
Zhengzhou University
2024
Jiangxi University of Science and Technology
2024
Shandong University
2024
Keck Hospital of USC
2022-2024
Minzu University of China
2024
Hebei University of Technology
2024
Background Human African trypanosomiasis (HAT) is an important public health problem in sub-Saharan Africa, affecting hundreds of thousands individuals. An urgent need exists for the discovery and development new, safe, effective drugs to treat HAT, as existing therapies suffer from poor safety profiles, difficult treatment regimens, limited effectiveness, a high cost goods. We have discovered optimized novel class small-molecule boron-containing compounds, benzoxaboroles, identify SCYX-7158...
The efficacy of reactive oxygen species (ROS)-related skin tumor therapies is significantly restricted by intracellular overexpressed glutathione (GSH) which a free radical scavenger. Herein, GSH-depleting and high ROS...
The recent development and spread of extensively drug-resistant totally resistant (TDR) strains Mycobacterium tuberculosis highlight the need for new antitubercular drugs. Protein synthesis inhibitors have played an important role in treatment (TB) starting with inclusion streptomycin first combination therapies. Although parenteral aminoglycosides are a key component therapy multidrug-resistant TB, oxazolidinone linezolid is only orally available protein inhibitor that effective against TB....
ABSTRACT We report the discovery of novel boron-containing molecules, exemplified by N -(1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)-2-trifluoromethylbenzamide (AN3520) and 4-fluoro- (SCYX-6759), as potent compounds against Trypanosoma brucei in vitro , including two subspecies responsible for human disease T. b. rhodesiense gambiense. These oxaborole carboxamides cured stage 1 (hemolymphatic) trypanosomiasis infection mice when administered orally at 2.5 to 10 mg/kg body weight 4...
Continuing structure-activity studies were performed on the 2,3,4, 5-tetrahydro-1-(imidazol-4-ylalkyl)-1,4-benzodiazepine farnesyltransferase (FT) inhibitors. These demonstrated that a 3(R)-phenylmethyl group, hydrophilic 7-cyano and 4-sulfonyl group bearing variety of substituents provide low-nanomolar FT inhibitors with cellular activity at concentrations below 100 nM. Maximal in vivo mutated K-Ras HCT-116 human colon tumor model was achieved analogues carrying hydrophobic side chains such...
ObjectivesThe objectives of this study were to determine species distribution and in vitro antifungal susceptibility Candida isolates identified the multicentre China-SCAN invasive infection (ICI) intensive care units (ICUs) across China.
A series of trisubstituted hydroxylactams was identified as potent enzymatic and cellular inhibitors human lactate dehydrogenase A. Utilizing structure-based design physical property optimization, multiple were discovered with <10 μM IC50 in a MiaPaca2 cell line. Optimization the led to 29, active molecule (MiaPaca2 = 0.67 μM) that also possessed good exposure when dosed orally mice.
Diverse biological roles for mitogen-activated protein kinase 4 (MAP4K4) have necessitated the identification of potent inhibitors in order to study its function various disease contexts. In particular, compounds that can be used carry out such studies vivo would critical elucidating potential therapeutic intervention. A structure-based design effort coupled with property-guided optimization directed at minimizing ability cross into CNS led an advanced compound 13 (GNE-495) showed excellent...
Abstract Objective: Osimertinib is the 3rd generation EGFR inhibitor, which has been approved for treatment of NSCLC patients with EGFRT790M. More recently, a tertiary EGFRC797S mutation was reported as dominant resistance (40~20%) mechanism to Osimertinib. The emergence C797S prevent covalent bond formation Osimertinib, and caused drug resistance. So, it’s an urgent demand new inhibitors that can effectively inhibit triple mutant, d746-750/T790M/C797S & L858R/T790M/C797S. Here, we...
Icariin as a hepatoprotector from Herba epimedii can expand the cardiovascular and cerebral blood vessels, promote hematopoietic functions, enhance immune system show anti-liver tumor activities. However, its low solubility (0.02 mg/mL) limits clinical applications food medical supplements. Through complexation with HP-γ-cyclodextrin by using trace amount of water-soluble polymer, water icariin was increased 654 times, which is best result to date for study icariin. In an in vitro...
This paper describes our studies aimed at the discovery of structurally distinct analogs cardioprotective KATP opener BMS-180448 (2) with improved selectivity for ischemic myocardium. The starting compound 6, derived from indole analog 4, showed good potency and excellent compared to 2 first-generation cromakalim (1). structure−activity indicate that increasing size alkyl ester leads diminished as does its replacement a variety other groups (nitrile, methyl sulfone). Replacement ethyl 6 an...