Search Results - "Lu, Zhonghui"
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1
Characteristics of Vegetation Photosynthesis under Flash Droughts in the Major Agricultural Areas of Southern China
Published in Atmosphere (01-08-2024)“…Flash droughts adversely affect agriculture and ecosystems due to their rapid depletion of soil moisture (SM). However, few studies assessed the impacts of…”
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2
Design, Synthesis and Antitumor Activity of Novel Selenium-Containing Tepotinib Derivatives as Dual Inhibitors of c-Met and TrxR
Published in Molecules (Basel, Switzerland) (30-01-2023)“…Cellular mesenchymal-epithelial transition factor (c-Met), an oncogenic transmembrane receptor tyrosine kinase (RTK), plays an essential role in cell…”
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3
Reliability and validity of the repetitive behavior scale-revised for young Chinese children with autism spectrum disorder in Jiangxi Province
Published in Frontiers in pediatrics (08-09-2022)“…Restricted and repetitive behaviors (RRBs) are one of the two main diagnostic features of autism spectrum disorder (ASD). To date, a growing body of research…”
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4
α,β-Cyclic-β-benzamido hydroxamic acids: Novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-α converting enzyme (TACE)
Published in Bioorganic & medicinal chemistry (15-01-2008)“…Selective inhibitors of TNF-α Converting Enzyme (TACE) based on novel α,β-cyclic-β-benzamido hydroxamic acids have been synthesized and evaluated. Selective…”
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5
Discovery of β-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors
Published in Bioorganic & medicinal chemistry (2008)“…β-Benzamido hydroxamic acids were discovered as potent TACE inhibitors. A computer model was constructed to help understanding the binding activities and…”
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6
Non-hydroxamate 5-phenylpyrimidine-2,4,6-trione derivatives as selective inhibitors of tumor necrosis factor-α converting enzyme
Published in Bioorganic & medicinal chemistry letters (15-06-2005)“…[Display omitted] New inhibitors of tumor necrosis factor-α converting enzyme (TACE) were discovered with a pyrimidine-2,4,6-trione in place of the commonly…”
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7
An unsupervised data mining-based framework for evaluation and optimization of operation strategy of HVAC system
Published in Energy (Oxford) (15-03-2024)“…The evaluation and optimization of existing operation strategies are significant for energy-saving in heating, ventilation, and air conditioning (HVAC)…”
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8
Discovery of N-Hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-α converting enzyme (TACE)
Published in Bioorganic & medicinal chemistry letters (16-06-2003)“…New inhibitors of tumor necrosis factor-α converting enzyme (TACE) were discovered using an N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamide scaffold. The series…”
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9
Population exposure to concurrent daytime and nighttime heatwaves in Huai River Basin, China
Published in Sustainable cities and society (01-10-2020)“…•Severe heatwaves are likely to occur in the southeastern parts of the basin.•Various indices of heatwaves show significant upward trends from 1987 to…”
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10
Design, Synthesis, and Antitumor Efficacy of Substituted 2‑Amino[1,2,4]triazolopyrimidines and Related Heterocycles as Dual Inhibitors for Microtubule Polymerization and Janus Kinase 2
Published in Journal of medicinal chemistry (09-11-2023)“…Preclinical and clinical studies have demonstrated the synergistic effect of microtubule-targeting agents in combination with Janus kinase 2 (JAK2) inhibitors,…”
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11
Anticancer efficacy triggered by synergistically modulating the homeostasis of anions and iron: Design, synthesis and biological evaluation of dual-functional squaramide-hydroxamic acid conjugates
Published in Bioorganic chemistry (01-06-2024)“…[Display omitted] •Dual-functional squaramide-hydroxamic acid conjugates were designed and synthesized.•Compound 16 exhibited potent antiproliferative activity…”
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12
Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches
Published in Journal of medicinal chemistry (10-12-2020)“…Scaffold hopping and structure-based drug design were employed to identify substituted 4-aminoquinolines and 4-aminonaphthyridines as potent, small molecule…”
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13
Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists
Published in ACS medicinal chemistry letters (14-03-2019)“…A new phenyl (3-phenylpyrrolidin-3-yl)sulfone series of RORγt inverse agonists was discovered utilizing the binding conformation of previously reported…”
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14
Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists
Published in Bioorganic & medicinal chemistry letters (15-06-2020)“…[Display omitted] Substituted benzyloxy aryl compound 2 was identified as an RORγt agonist. Structure based drug design efforts resulted in a potent and…”
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15
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists
Published in Bioorganic & medicinal chemistry letters (15-08-2019)“…[Display omitted] An X-ray crystal structure of one of our previously discovered RORγt inverse agonists bound to the RORγt ligand binding domain revealed that…”
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16
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity
Published in Bioorganic & medicinal chemistry letters (15-01-2018)“…[Display omitted] We disclose the optimization of a high throughput screening hit to yield benzothiazine and tetrahydroquinoline sulfonamides as potent RORγt…”
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17
Discovery of highly potent, selective, covalent inhibitors of JAK3
Published in Bioorganic & medicinal chemistry letters (15-10-2017)“…[Display omitted] A useful and novel set of tool molecules have been identified which bind irreversibly to the JAK3 active site cysteine residue. The design…”
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Discovery of 2,6–difluorobenzyl ether series of phenyl ((R)–3–phenylpyrrolidin–3–yl)sulfones as surprisingly potent, selective and orally bioavailable RORγt inverse agonists
Published in Bioorganic & medicinal chemistry letters (01-10-2020)“…[Display omitted] In an effort to discover oral inverse agonists of RORγt to treat inflammatory diseases, a new 2,6–difluorobenzyl ether series of cyclopentyl…”
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19
Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors
Published in Bioorganic & medicinal chemistry letters (15-07-2017)“…[Display omitted] A series of potent dual JAK1/3 inhibitors have been developed from a moderately selective JAK3 inhibitor. Substitution at the C6 position of…”
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20
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors
Published in Bioorganic & medicinal chemistry letters (15-12-2014)“…A new class of Janus kinase (JAK) inhibitors was discovered using a rationally designed pyrrolo[1,2-b]pyridazine-3-carboxamide scaffold. Preliminary studies…”
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