Search Results - "Zhuo, Linsheng"
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Discovery of 8-Amino-Substituted 2-Phenyl-2,7-Naphthyridinone Derivatives as New c-Kit/VEGFR-2 Kinase Inhibitors
Published in Molecules (Basel, Switzerland) (05-12-2019)“…The 2,7-naphthyridone scaffold has been proposed as a novel lead structure of MET inhibitors by our group. To broaden the application of this new scaffold, a…”
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Development of o -aminobenzamide salt derivatives for improving water solubility and anti-undifferentiated gastric cancer
Published in Frontiers in pharmacology (11-07-2023)“…Gastric cancer is one of the cancers with wide incidence, difficult treatment and high mortality in the world, especially in Asia and Africa. In our previous…”
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From tryptamine to the discovery of efficient multi-target directed ligands against cholinesterase-associated neurodegenerative disorders
Published in Frontiers in pharmacology (28-11-2022)“…A novel class of benzyl-free and benzyl-substituted carbamylated tryptamine derivatives (CDTs) was designed and synthesized to serve as effective building…”
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Novel N-phenyl-2-(aniline) benzamide hydrochloride salt development for colon cancer therapy
Published in Frontiers in pharmacology (30-10-2024)“…Introduction N -phenyl-2-(aniline) analog N53 is a previously discovered dual inhibitor of Topo I and COX-2, which exhibited significant anti-colon cancer…”
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Discovery of pyrrole derivatives as acetylcholinesterase-sparing butyrylcholinesterase inhibitor
Published in Frontiers in pharmacology (06-12-2022)“…Inspired by the crucial roles of (hetero)aryl rings in cholinesterase inhibitors and the pyrrole ring in new drug discovery, we synthesized 19 pyrrole…”
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Auto In Silico Ligand Directing Evolution to Facilitate the Rapid and Efficient Discovery of Drug Lead
Published in iScience (26-06-2020)“…Motivated by the growing demand for reducing the chemical optimization burden of H2L, we developed auto in silico ligand directing evolution…”
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Natural product evodiamine-inspired medicinal chemistry: Anticancer activity, structural optimization and structure-activity relationship
Published in European journal of medicinal chemistry (05-02-2023)“…It is a well-known phenomenon that natural products can serve as powerful drug leads to generate new molecular entities with novel therapeutic utility…”
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Recent advance on pleiotropic cholinesterase inhibitors bearing amyloid modulation efficacy
Published in European journal of medicinal chemistry (15-11-2022)“…Due to the hugely important roles of neurotransmitter acetylcholine (ACh) and amyloid-β (Aβ) in the pathogenesis of Alzheimer's disease (AD), the development…”
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Discovery of 7-(1-methyl-1H-pyrazol-4-yl)-1,6-naphthyridine derivatives as potent inhibitors of rearranged during transfection (RET) and RET solvent-front mutants for overcoming selpercatinib resistance
Published in European journal of medicinal chemistry (05-12-2024)“…Rearranged during transfection kinase (RET) inhibition has been considered a promising therapeutic approach for treatment of a variety of cancers. However, the…”
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Discovery of N-substituted-3-phenyl-1,6-naphthyridinone derivatives bearing quinoline moiety as selective type II c-Met kinase inhibitors against VEGFR-2
Published in Bioorganic & medicinal chemistry (15-06-2020)“…[Display omitted] •N-substituted 1,6-naphthyridinones was identified as new MET inhibitor.•Lead compound 4r displayed promising selectivity against…”
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Structure-activity relationship study of 1,6-naphthyridinone derivatives as selective type II AXL inhibitors with potent antitumor efficacy
Published in European journal of medicinal chemistry (05-02-2024)“…The role of AXL in various oncogenic processes has made it an attractive target for cancer therapy. Currently, kinase selectivity profiles, especially…”
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Fenamates: Forgotten treasure for cancer treatment and prevention: Mechanisms of action, structural modification, and bright future
Published in Medicinal research reviews (22-08-2024)“…Fenamates as classical nonsteroidal anti-inflammatory agents are widely used for relieving pain. Preclinical studies and epidemiological data highlight their…”
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Discovery of carbamate-based salicylic acid derivatives as novel cholinesterase inhibitor
Published in Journal of molecular structure (15-03-2023)“…•20 novel salicylic acid carbamate derivatives were synthesized for the systematical structure-activity relationship studies.•Compounds 3l and 3t are…”
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N(14)-substituted evodiamine derivatives as dual topoisomerase 1/tubulin-Inhibiting anti-gastrointestinal tumor agents
Published in European journal of medicinal chemistry (05-07-2023)“…Gastrointestinal tumor is an important factor threatening human health. Natural product-based drug discovery is a popular paradigm for expanding the chemical…”
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Design, synthesis, and biological evaluation of 1-styrenyl isoquinoline derivatives for anti-hepatocellular carcinoma activity and effect on mitochondria
Published in European journal of medicinal chemistry (05-08-2023)“…In this study, 18 derivatives of 1-styrene-isoquinoline were designed and synthesized from resveratrol and isoquinoline. The IC50 of compound 1c against Huh7…”
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Design, synthesis and biological evaluation of N-salicyloyl tryptamine derivatives as multifunctional neuroprotectants for the treatment of ischemic stroke
Published in European journal of medicinal chemistry (15-11-2024)“…Ischemic stroke (IS) is a disease of high death and disability worldwide with few medications in clinical treatment. Neuroinflammation and oxidative stress are…”
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Identification of a novel 10-hydroxyevodiamine prodrug as a potent topoisomerase inhibitor with improved aqueous solubility for treatment of hepatocellular carcinoma
Published in European journal of medicinal chemistry (05-12-2024)“…Natural product evodiamine (Evo) and its synthetic derivatives represent an attractive dual Topo 1/2 inhibitors with broad-spectrum antitumor efficacy…”
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Discovery of novel small molecules targeting the USP21/JAK2/STAT3 axis for the treatment of triple-negative breast cancer
Published in European journal of medicinal chemistry (05-07-2024)“…The deficiency in available targeted agents and frequency of chemoresistance are primary challenges in clinical management of triple-negative breast cancer…”
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Exploring the Therapeutic Effects of Multifunctional N‑Salicylic Acid Tryptamine Derivative against Parkinson’s Disease
Published in ACS omega (08-08-2023)“…Parkinson’s disease (PD) is the second most common neurodegenerative disease worldwide. Neuroinflammation and oxidative stress play an important role in the…”
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Design, synthesis and evaluation of highly selective pyridone-based class II MET inhibitors
Published in Bioorganic & medicinal chemistry letters (01-08-2014)“…The high incidence of MET oncogene activation in human malignancies has prompted researchers to develop MET inhibitors. As part of our efforts to developing…”
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