A5102721405- Click Chemistry and Applications
- Synthesis and Biological Evaluation
- Tryptophan and brain disorders
- Lung Cancer Treatments and Mutations
- Peptidase Inhibition and Analysis
- Cancer therapeutics and mechanisms
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and biological activity
- Quinazolinone synthesis and applications
- Cancer-related gene regulation
- HIV Research and Treatment
- Receptor Mechanisms and Signaling
- Biochemical and Molecular Research
- Pharmacological Receptor Mechanisms and Effects
- Immune cells in cancer
- Synthesis and Characterization of Heterocyclic Compounds
- Nanoplatforms for cancer theranostics
- Chronic Lymphocytic Leukemia Research
- Bipolar Disorder and Treatment
- HIV/AIDS drug development and treatment
- Fungal Plant Pathogen Control
- Synthesis of Organic Compounds
- Neuroscience and Neuropharmacology Research
- Treatment of Major Depression
- Antimicrobial Peptides and Activities
Henan University of Science and Technology
2022-2025
Luye Pharma (China)
2024
Henan Normal University
2014-2024
Nankai University
2020-2023
State Key Laboratory of Medicinal Chemical Biology
2020-2023
Ministère de l'Agriculture et de la Souveraineté alimentaire
2023
Shandong Academy of Agricultural Sciences
2023
First Affiliated Hospital of Henan University of Science and Technology
2016-2022
Institute of Agro-Products Processing Science and Technology
2022
Abstract A series of 20 novel gefitinib derivatives incorporating the 1,2,3-triazole moiety were designed and synthesized. The synthesized compounds evaluated for their potential anticancer activity against EGFR wild-type human non-small cell lung cancer cells (NCI-H1299, A549) adenocarcinoma (NCI-H1437) as cancer. In comparison to gefitinib, Initial biological assessments revealed that several exhibited potent anti-proliferative these lines. Notably, 7a 7j demonstrated most pronounced...
Given the potent anti-inflammatory properties of 1,2,3-triazole structure and wide use 2H-1,4-benzoxazin-3(4H)-one in developing treatments for neurodegenerative diseases, a series derivatives were synthesized by introducing moiety. Screening activity microglial cells revealed that compounds e2, e16, e20 exhibited most promising effects without significant cytotoxicity. These effectively reduced LPS-induced NO production significantly decreased transcription levels pro-inflammatory cytokines...
Abstract Indoleamine 2,3-dioxygenase 1 (IDO1) is an immunomodulatory enzyme associated with tumor immune evasion, making it a promising target for cancer therapy. This study aimed to identify novel holo-IDO1 inhibitors distinct structural scaffolds. A series of theophylline derivatives containing 1,2,3-triazole groups were designed and synthesized through the condensation acetic acid 4-aminophenylacetylene. Among compounds, 3c 3e exhibited most potent inhibitory effects in IDO1 enzymatic...
ABSTRACT Aims Advanced cancer patients frequently endure severe pain from bone metastases, and few effective treatments for (BCP) exist. Although Anwulignan is known its antioxidant, anti‐inflammatory, antitumor properties, effects on BCP remain unclear. This study aims to explore the analgesic mechanisms of pain. Methods Western blotting immunofluorescence assessed molecular expression localization. X‐ray, micro‐CT, TRAP, ALP staining examined destruction in rats. MTT, colony formation...
Bruton's tyrosine kinase (BTK) inhibitors suppressing the aberrant activation of BTK have led to a paradigm shift in therapy B-cell malignancies. However, there is an urgent need discover more selective covalent owing off-target adverse effects approved inhibitor, ibrutinib. Herein, we disclose discovery and preliminary activity studies novel carrying 1-amino-1H-imidazole-5-carboxamide as hinge binder. The most potent inhibitor 26 demonstrates impressive selectivity, favorable...
The theophylline derivative d17 is a candidate drug for nonsmall cell lung cancer (NSCLC) treatment previously developed by our group. However, it has the limitations of inadequate bioavailability, poor targeting, and insignificant therapeutic effect. Chemo-photodynamic synergistic therapy promising method antitumor therapy. Herein, photosensitizer chlorin e6 (Ce6) were loaded into nanoparticles (NPs) via supramolecular self-assembly, which are self-assembled through π–π stacking hydrogen...
Graphical Abstract
A series of 28 novel cabotegravir derivatives, incorporating the 1,2,3-triazole moiety, were designed and synthesized. The synthesized compounds evaluated for their potential anticancer activity against four different human cancer cell lines: HuH-7 (hepatocellular), MCF-7 (breast), SKOV3 (ovarian), HCT-116 (colon). Initial biological assessments revealed that several exhibited potent anti-proliferative these lines. Notably, KJ9 KJ23 demonstrated most pronounced effects, with IC50 values 6.59...
Tumor immunotherapy is considered to be a highlight in cancer treatment recent years. Indoleamine 2,3-dioxygenase 1 (IDO1) closely related the over expression of many cancers, and therefore promising target for tumor immunotherapy. To search novel IDO1-targeting therapeutic agents, 22 icotinib-linked 1,2,3-triazole derivatives were prepared evaluated their inhibitory activity against IDO1. The structures compounds confirmed with1H NMR, 13C NMR HR MS. IDO1 assay results indicated that 10...
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) are emerging at the vanguard of therapy for non-small-cell lung cancer (NSCLC) patients with EGFR-activating mutations. However, increasing therapeutic resistance caused by novel mutations or activated bypass pathways has impaired their performance. In this study, we link one commercial EGFR-TKIs, Erlotinib, to different azide compounds synthesize a class 1,2,3-triazole ring-containing Erlotinib derivatives. We...
Nineteen erlotinib derivatives bearing different 1,2,3-triazole moieties were designed, synthesized, and evaluated for their potential against cancer cell lines. The structures of the synthesized compounds confirmed via 1 H NMR, 13 C HR MS. Preliminary antitumor activity assay results suggested that some showed remarkable inhibitory lines including corresponding drug-resistant ones. Among these compounds, 3d was most promising one with an IC 50 7.17 ± 0.73 μM (KYSE70TR), 7.91 0.61...
In this study, acenaphthylene was used as the raw material, and a series of novel 1,8-naphthalimide-1,2,3-triazole derivatives obtained through oxidation, acylation, alkylation, click reactions, subsequently, their anti-tumor activities were tested. After screening, we found that Compound 5e showed good activity against H1975 lung cancer cells, with half maximal inhibitory concentration (IC 50 ) reaching 16.56 μM.
Chemotherapy is the most common clinical treatment for non-small cell lung cancer (NSCLC), but low efficiency and high toxicity of current chemotherapy drugs limit their application. Therefore, it urgent to develop hypotoxic efficient drugs. Theophylline, a natural compound, safe easy get, can be used as modified scaffold structure hold huge potential developing antitumor Herein, we linked theophylline with different azide compounds synthesize new type 1,2,3-triazole ring-containing...
Indoleamine 2,3-dioxygenase 1 (IDO1) has received much attention as an immunomodulatory enzyme in the field of cancer immunotherapy. While several IDO1 inhibitors have entered clinical trials, there are currently no inhibitor drugs on market. To explore potential inhibitors, we designed a series compounds with urea and 1,2,3-triazole structures. Organic synthesis enzymatic activity experiments verified molecular-level activities compounds, IC50 value compound 3a was 0.75 μM. Molecular...
Indoleamine 2,3-dioxygenase 1 (IDO1) has attracted much attention in the field of cancer immunotherapy as an immunomodulatory enzyme. To identify potential IDO1 inhibitors, a novel series compounds with N,N-diphenylurea and triazole structures were synthesized. The designed underwent organic synthesis, subsequent enzymatic activity experiments targeting confirmed their at molecular level. These provided validation for efficacy inhibiting IDO1, compound 3g exhibited IC50 value 1.73 ± 0.97 μM....
Abstract A series of indirubin derivatives hydrochloride were obtained using a convenient and mild method from indirubin. The newly synthesized compounds their characterized by 1 H NMR, 13 C MS. Furthermore, we tested IDO1 enzyme inhibitory activity anti‐proliferative activities in K562 tumor cells. experimental results revealed that some the showed potential anti‐enzyme anti‐tumor activity. Among them, compound 4b exhibited certain on (IC 50 : 29.52 μmol/L), 4a displayed similar to cells...
Previous report showed that a variety of icotinib derivatives bearing different 1,2,3-triazole moieties, which could be readily prepared
In order to obtain novel bioactive compounds with significant antifungal activities, a series of 2H-1,4-benzoxazin-3(4H)-one analogs linked 1,2,3-triazole moiety have been designed and synthesized via click reactions in one-pot process at room temperature using CuCl as the catalyst. Their activities were tested against two plant-pathogenic fungi, Rhizoctonia cerealis (RC) Colletotrichum capsici (CC). Statistical analysis showed that among particular compound 3a exhibits growth inhibitory...
Abstract In order to find novel bioactive compounds with significant antifungal activities, a series of 1,4-disubstituted 1,2,3-triazoles containing an indole ring via CuCl 2 /Zn-catalyzed Huisgen cycloaddition were designed, synthesized, and characterized. Antifungal activity against colletotrichum capsici cotton physalospora pathogens all the prepared was evaluated, test results indicated that these compounds, especially 4g 4h , showed inhibitory effects for fungi. All synthesized have...
Mirabegron is a muscle relaxing drug for the treatment of overactive bladder. The existing synthetic methods mirabegron produced intermediate product 4‐(2‐(phenethylamino)ethyl)aniline, which complicated final purification process. In this study, we designed new route with low cost starting materials and production at 99.6% purity 61% overall yield. Particularly, did not produce side significantly simplified