A5101962195- Nanoplatforms for cancer theranostics
- Piperaceae Chemical and Biological Studies
- Histone Deacetylase Inhibitors Research
- Phytochemical compounds biological activities
- Cholinesterase and Neurodegenerative Diseases
- Luminescence and Fluorescent Materials
- Synthesis and Biological Activity
- Antimicrobial Peptides and Activities
- Synthesis and biological activity
- Peptidase Inhibition and Analysis
- Immune cells in cancer
- Catalytic Alkyne Reactions
- Genomics, phytochemicals, and oxidative stress
- Advanced biosensing and bioanalysis techniques
- Chemical Synthesis and Reactions
- Synthesis and Biological Evaluation
- Protein Degradation and Inhibitors
- Supramolecular Chemistry and Complexes
- Asymmetric Hydrogenation and Catalysis
- Enzyme function and inhibition
- Cancer Mechanisms and Therapy
- Glutathione Transferases and Polymorphisms
- Phenothiazines and Benzothiazines Synthesis and Activities
- Supramolecular Self-Assembly in Materials
- Cancer Treatment and Pharmacology
China Pharmaceutical University
2025
Nantong University
2018-2024
Target (United States)
2021
Nantong Science and Technology Bureau
2021
Affiliated Hospital of Nantong University
2020
Zhejiang University of Technology
2009-2011
Chemotherapy-induced myelosuppression (CIM) significantly impairs hematopoiesis. Trilaciclib (TC), originally developed for oncology application, is the only FDA-approved CDK4/6 inhibitor CIM, which effectively protects bone marrow cells by inhibiting their proliferation. In this study, a series of TC derivatives were designed and synthesized as inhibitors (CDK4/6i) alleviating CIM. Among these, 42 displayed potent inhibitory activity (IC50 = 11 nM), lower cytotoxicity (CC50 > 100 μM) showed...
Naturally occurring β-carbolines are known to have antitumor activities but with limited effectiveness. In order improve their efficacy, a series of new hydroxamic-acid-containing connected via hydroxycinnamic acid moitey (12a–f) were developed incorporate histone deacetylase (HDAC) inhibition for possible synergistic effects. When evaluated in vitro assays, most the analogues showed significant against four human cancer cells. particular, 12b highest cytotoxic potency series, including...
The natural products piperlongumine and piperine have been shown to inhibit cancer cell proliferation through elevation of reactive oxidative species (ROS) eventually death, but only modest cytotoxic potencies. A series 14 novel phenylallylidenecyclohexenone analogues based on therefore were designed synthesized, their pharmacological properties evaluated. Most the compounds produced antiproliferative activities against five human cells with IC50 values lower than those piperine. Among...
Two novel theranostic agents HJTA and HJTB have been designed synthesized by covalently linking a β-carboline derivative, with antitumor activities pH-responsive fluorescence, 2-exomethylenecyclohexanone moiety, which can be activated the tumor-targeting glutathione (GSH)/glutathione S-transferase π (GSTπ). These showed pH- GSH-dual-responsive fluorescence in tumor cells but not normal cells. Importantly, selectively illuminated tissue for up to 7 h generated precise visualization of...
Chemodynamic therapy (CDT) based on the intracellular Fenton reaction has become increasingly explored in cancer treatment. However, mildly acidic tumor microenvironment and limited amount of hydrogen peroxide (H2O2) will create issues for CDT to perform a sustained high-efficiency Therefore, how selectively reduce pH value augment H2O2 tissues key factor realizing excellent CDT. Besides, majority reported systems have been constructed from iron-based inorganic or metal-organic framework...
A large number of pyrazole derivatives have different biological activities such as anticancer, antimicrobial, anti-inflammatory, analgesic and antiepileptic activity. Among them, oximes attracted much attention due to their potential pharmacological activities, particularly anticancer activities.Our goal is synthesize novel thiazolyl substituted bis-pyrazole oxime with potent antitumor by selectively inducing apoptosis Reactive Oxygen Species (ROS) accumulation in cancer cells.Eighteen were...
The natural products piperlongumine (1) and ligustrazine (2) have been reported to exert antiproliferative effects against various types of cancer cells by up-regulating the level reactive oxidative species (ROS). However, moderate activities 1 2 limit their application. To improve potential antitumor activity, novel piperlongumine/ligustrazine derivatives were designed prepared, pharmacological determined in vitro vivo. Among obtained, 11 exerted more prominent inhibitory proliferation...
A novel theranostic co-prodrug SCB has been designed by combining a from CDDO-Me and SAHA with biotin-coupled near-infrared (NIR) probe hemicyanine via redox-responsive linker thiolactate to enhance the tumor efficacy reduce toxic side effects using both active passive targeting strategies. displayed reactive oxygen species (ROS)- glutathione (GSH)-dependent release of NIR fluorescence two parent drugs. Furthermore, administration caused selective illumination tissues for >24 h, thereby...
Either [1,3]- or [3,3]-sigmatropic rearrangements were selectively accessed by controlling the reaction temperature in gold(III)-catalyzed tandem rearrangement/cyclization of (E)-2-(aryloxymethyl)alk-2-enoates to afford diversely substituted 3,4-dihydrocoumarin derivatives moderate good yields and excellent regioselectivity.
Abstract The natural product piperlonguminine (PL) has been shown to exert potential anticancer activity against several types of cancer via elevation reactive oxidative species (ROS). However, the application PL limited due its poor water solubility and moderate activity. To improve PL's potency, we designed synthesized a series 17 novel phenylmethylenecyclohexenone derivatives evaluated their pharmacological properties. Most them exerted antiproliferative activities four cell lines with IC...
Chemodynamic therapy (CDT) based on intracellular Fenton reactions is attracting increasing interest in cancer treatment. A simple and novel method to regulate the tumor microenvironment for improved CDT with satisfactory effectiveness urgently needed. Therefore, glutathione (GSH)/ROS (reactive oxygen species) dual-responsive supramolecular nanoparticles (GOx@BNPs) chemo-chemodynamic combination were constructed via host-guest complexation between water-soluble pillar[6]arene...
The accurate diagnosis and effective therapy of malignant tumors is still a challenge owing to its poor prognosis, recurrence, drug resistance. In this study, tumor microenvironment responsive high O2-economic effect nano-theranostic agent GOx@NPs was constructed through the self-assembly GOx CDDO-Fe, which synthesized by coupling natural chemotherapeutic CDDO-Me blocked ferrocene (Fc) with near-infrared (NIR) fluorescence probe hemicyanine (I-CyOH) via redox-responsive linker...
Given that precise/rapid intraoperative tumor margin identification is still challenging, novel fluorescent probes HY and HYM, based on acidic microenvironment (TME) activation organic anion transporting polypeptide (OATPs)-mediated selective uptake, were constructed synthesized. Both of them possessed pH-activatable reversible fluorescence as well large Stokes shift. Compared with HY, HYM had a higher (over 9-fold) enhancement in pH ranging from 7.6 to 4.0, the quantum yield (ΦF = 0.49) at...
Tumor microenvironment-triggered supramolecular nanosystems were fabricated, which showed excellent ability in cancer precision diagnosis and synergistic therapy.
Objectives: The development of novel long-acting injectables for local anesthetics is necessary to effectively manage the acute postoperative pain. aim this study was prepare an injectable oil-based formulation ropivacaine (ROP) prodrug (ropivacaine stearoxil, ROP-ST) and investigate pharmacokinetics pharmacodynamics after administration. Methods: A N-acyloxymethyl ROP, i.e., ROP-ST, synthesized its physicochemical properties such as log P, solubility stability characterized. soybean depot...