Search Results - "Chu, Zhaoxing"
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Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3‑Kinase Inhibitors as a Promising Strategy for Cancer Therapy
Published in Journal of medicinal chemistry (09-01-2020)“…Concomitant inhibition of PARP and PI3K pathways has been recognized as a promising strategy for cancer therapy, which may expand the clinical utility of PARP…”
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Regorafenib-loaded poly (lactide-co-glycolide) microspheres designed to improve transarterial chemoembolization therapy for hepatocellular carcinoma
Published in Asian journal of pharmceutical sciences (01-11-2020)“…Transarterial chemoembolization (TACE) has been widely introduced to treat hepatocellular carcinoma (HCC) especially for unresectable patients for decades…”
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Semi-Mechanistic Modeling of HY-021068 Based on Irreversible Inhibition of Thromboxane Synthetase
Published in Frontiers in pharmacology (30-11-2020)“…HY-021068 [4-(2-(1H-imidazol-1-yl) ethoxy)-3-methoxybenzoate], developed by Hefei Industrial Pharmaceutical Institute Co., Ltd. (Anhui, China), is a potential…”
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Phase I Trial of Pyragrel, a Novel Thromboxane Synthetase Inhibitor, to Evaluate the Safety, Tolerability, and Pharmacokinetics in Healthy Volunteers
Published in Frontiers in pharmacology (24-10-2019)“…Background and Objective: Inhibition of thrombosis and platelet aggregation through a thromboxane synthetase inhibitor proved to be an effective and promising…”
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Li, P HY-021068 alleviates cerebral ischemia-reperfusion injury by inhibiting NLRP1 inflammasome and restoring autophagy function in mice
Published in Experimental neurology (01-01-2024)“…Cerebral ischemia-reperfusion injury (CIRI) is a severe pathological condition that involves oxidative stress, inflammatory response, and neuronal damage…”
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Synthesis and biological evaluation of N-(benzene sulfonyl)acetamide derivatives as anti-inflammatory and analgesic agents with COX-2/5-LOX/TRPV1 multifunctional inhibitory activity
Published in Bioorganic & medicinal chemistry letters (15-01-2023)“…[Display omitted] •A series of novel N- (benzene sulfonyl) acetamide derivatives were designed and synthesized.•9a and 9b showed significant suppressive…”
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Discovery of the First Potent IDO1/IDO2 Dual Inhibitors: A Promising Strategy for Cancer Immunotherapy
Published in Journal of medicinal chemistry (23-12-2021)“…Indoleamine 2,3-dioxygenase-1 (IDO1) plays an important role in tumor immune escape. However, unsatisfactory clinical efficacies of selective IDO1 inhibitors…”
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Liquiritin Attenuates Angiotensin II-Induced Cardiomyocyte Hypertrophy via ATE1/TAK1-JNK1/2 Pathway
Published in Evidence-based complementary and alternative medicine (2022)“…Objective. To investigate the protective effect and mechanism of liquiritin (LIQ) on cardiomyocyte hypertrophy induced by angiotensin II (Ang II). Methods…”
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Preclinical pharmacokinetic investigation of the bioavailability and skin distribution of HY-072808 Ointment, a novel drug candidate for the treatment of atopic dermatitis, in minipigs by a newly LC-MS/MS method
Published in Xenobiotica (15-03-2024)“…1. HY-072808 is a novel phosphodiesterase 4 inhibitor clinically used for topical atopic dermatitis treatment. Cytochrome P450 enzymes are involved in…”
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Discovery of novel brain-penetrant GluN2B NMDAR antagonists via pharmacophore-merging strategy as anti-stroke therapeutic agents
Published in European journal of medicinal chemistry (05-01-2022)“…In this work, a novel structural series of brain-penetrant GluN2B NMDAR antagonists were designed, synthesized and biologically evaluated as anti-stroke…”
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Design, Synthesis, and Biological Evaluation of Pierardine Derivatives as Novel Brain-Penetrant and In Vivo Potent NMDAR-GluN2B Antagonists for Ischemic Stroke Treatment
Published in Journal of medicinal chemistry (14-03-2024)“…A series of structurally novel GluN2B NMDAR antagonists were designed, synthesized, and biologically evaluated as anti-stroke therapeutics by optimizing the…”
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Design, synthesis and biological evaluation of novel benzoxaborole derivatives as potent PDE4 inhibitors for topical treatment of atopic dermatitis
Published in European journal of medicinal chemistry (05-03-2021)“…In this work, a series of structurally novel benzoxaborole derivatives were designed, synthesized and biologically evaluated as PDE4 inhibitors for battling…”
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Discovery of the First Selective IDO2 Inhibitor As Novel Immunotherapeutic Avenues for Rheumatoid Arthritis
Published in Journal of medicinal chemistry (10-11-2022)“…Indoleamine 2,3-dioxygenase 2 (IDO2), a closely related homologue of well-studied immunomodulatory enzyme IDO1, has been identified as a pathogenic mediator of…”
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Discovery of the novel and potent histamine H1 receptor antagonists for treatment of allergic diseases
Published in European journal of medicinal chemistry (15-03-2024)“…Desloratadine, a second-generation histamine H1 receptor antagonist, has established itself as a first-line drug for the treatment of allergic diseases…”
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LC–MS/MS determination of HY072808, a novel candidate for treating atopic dermatitis, and its active metabolite: Application to a first‐in‐human pharmacokinetic study
Published in Biomedical chromatography (01-02-2023)“…HY072808 is a novel phosphodiesterase 4 inhibitor currently under clinical development to treat atopic dermatitis. The first step is to address the…”
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Design, synthesis and biological evaluation of novel desloratadine derivatives with anti-inflammatory and H1 antagonize activities
Published in Bioorganic & medicinal chemistry letters (15-12-2019)“…To improve the anti-inflammatory activity of desloratadine, we designed and synthesized a series of novel desloratadine derivatives. All compounds were…”
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In vitro and Ex vivo Antioxidant Activity and Sustained Release Properties of Sinomenine-Loaded Liposomes-in-Hydrogel Biomaterials Simulating Cells-in-Extracellular Matrix
Published in Natural product communications (01-11-2022)“…Sinomenine (SIN), a natural product, has been used to treat rheumatoid arthritis (RA) in China for thousands of years. SIN has been developed for the treatment…”
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Design, synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors
Published in Bioorganic & medicinal chemistry letters (01-04-2013)“…A series of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP inhibitors is described. A series of novel cyclic amine-substituted…”
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Profiling and Preparation of Metabolites from Pyragrel in Human Urine by Online Solid-Phase Extraction Coupled with High Performance Liquid Chromatography Tandem Mass Spectrometry Followed by a Macroporous Resin-Based Purification Approach
Published in Molecules (Basel, Switzerland) (21-03-2017)“…Pyragrel, a new anticoagulant drug, is derived from the molecular combination of ligustrazine and ferulic acid. Pyragrel showed significant inhibitory activity…”
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