Linxiang Zhao
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View article: Harnessing regioselective aryl migration of pyridone-based aryl-λ3‑iodonium salts to access iodine-substituted aryloxypyridines
Harnessing regioselective aryl migration of pyridone-based aryl-λ3‑iodonium salts to access iodine-substituted aryloxypyridines Open
While 2- and 4-aryloxypyridines are ubiquitous in pharmaceutical molecules, efficient synthetic strategies—especially for synthesizing scaffolds with diverse multiple substituents on the pyridine core—remain limited. Here we report a hook-…
View article: Targeting aerobic glycolysis combats tyrosine kinase inhibitor resistance of hepatocellular carcinoma
Targeting aerobic glycolysis combats tyrosine kinase inhibitor resistance of hepatocellular carcinoma Open
Hepatocellular carcinoma (HCC) represents the predominant form of primary liver cancer and is frequently identified at a late stage, necessitating systemic therapy. However, resistance to first‐line tyrosine kinase inhibitor therapies, suc…
View article: Publisher Correction: Nonheme Fe 1,3-nitrogen migratases for asymmetric noncanonical amino acid synthesis
Publisher Correction: Nonheme Fe 1,3-nitrogen migratases for asymmetric noncanonical amino acid synthesis Open
View article: The MASTL/YBX1/PAK4 axis regulated by stress-activated STK24 triggers lenvatinib resistance and tumor progression in HCC
The MASTL/YBX1/PAK4 axis regulated by stress-activated STK24 triggers lenvatinib resistance and tumor progression in HCC Open
Background and Aims: Many patients with HCC present inadequate responses to lenvatinib therapy. Therefore, it is important to elucidate the underlying mechanisms of resistance and to formulate effective reversal strategies. Approach and Re…
View article: Cooperative Photometallobiocatalysis: Nonheme Fe Enzyme‐Catalyzed Enantioconvergent Radical Decarboxylative Azidation, Thiocyanation, and Isocyanation of Redox‐Active Esters
Cooperative Photometallobiocatalysis: Nonheme Fe Enzyme‐Catalyzed Enantioconvergent Radical Decarboxylative Azidation, Thiocyanation, and Isocyanation of Redox‐Active Esters Open
Cooperative catalysis with an enzyme and a small‐molecule photocatalyst has recently emerged as a potentially general activation mode to advance novel biocatalytic reactions with synthetic utility. Herein, we report cooperative photobiocat…
View article: Cooperative Photometallobiocatalysis Enables Nonheme Fe Enzyme-Catalyzed Enantioconvergent Radical Decarboxyla-tive Azidation, Thiocyanation and Isocyanation of Redox-Active Esters
Cooperative Photometallobiocatalysis Enables Nonheme Fe Enzyme-Catalyzed Enantioconvergent Radical Decarboxyla-tive Azidation, Thiocyanation and Isocyanation of Redox-Active Esters Open
Cooperative catalysis with an enzyme and a small-molecule photocatalyst has very recently emerged as a potentially general activation mode to advance novel biocatalytic reactions with synthetic utility. Herein, we report cooperative photob…
View article: Discovery of 4,5-Dihydro-Benzo[G]Indazole-Based Hydroxamic Acids as Hdac3/Brd4 Dual Inhibitors and Anti-Tumor Agents
Discovery of 4,5-Dihydro-Benzo[G]Indazole-Based Hydroxamic Acids as Hdac3/Brd4 Dual Inhibitors and Anti-Tumor Agents Open
View article: Construction of Diversified Penta‐Spiro‐Heterocyclic and Fused‐Heterocyclic Frameworks with Potent Antitumor Activity
Construction of Diversified Penta‐Spiro‐Heterocyclic and Fused‐Heterocyclic Frameworks with Potent Antitumor Activity Open
Invited for the cover of this issue are Xuewu Liang, Hong Liu and co‐workers at the Shanghai Institute of Materia Medica and Shenyang Pharmaceutical University. The image depicts how a rhodium‐catalyzed methodology leads to novel penta‐spi…
View article: Front Cover: Construction of Diversified Penta‐Spiro‐Heterocyclic and Fused‐Heterocyclic Frameworks with Potent Antitumor Activity (Chem. Eur. J. 54/2023)
Front Cover: Construction of Diversified Penta‐Spiro‐Heterocyclic and Fused‐Heterocyclic Frameworks with Potent Antitumor Activity (Chem. Eur. J. 54/2023) Open
Four novel types of complicated penta-spiro/fused-heterocyclic frameworks based on an indazolone scaffold have been constructed by C−H activation/[4+1] and [4+2] annulation cascades. The novel spiro[cyclohexane-indazolo[1,2-a]indazole] fra…
View article: Small molecules targeting γ-secretase and their potential biological applications
Small molecules targeting γ-secretase and their potential biological applications Open
View article: Studying Histone Deacetylase Inhibition and Apoptosis Induction of Psammaplin A Monomers with Modified Thiol Group
Studying Histone Deacetylase Inhibition and Apoptosis Induction of Psammaplin A Monomers with Modified Thiol Group Open
Psammaplin A (PsA) is a bromotyrosine disulfide dimer with histone deacetylase (HDAC) inhibition and acts through reduced monomer PsA-SH. We studied the connection of HDAC inhibition, cell growth inhibition, and apoptosis induction of PsA-…
View article: Design, Synthesis and Bioactivity Evaluation of 4,6-Disubstituted Pyrido[3,2-d]pyrimidine Derivatives as Mnk and HDAC Inhibitors
Design, Synthesis and Bioactivity Evaluation of 4,6-Disubstituted Pyrido[3,2-d]pyrimidine Derivatives as Mnk and HDAC Inhibitors Open
Both HDACs and Mnks play important role in translating multiple oncogenic signaling pathways during oncogenesis. As HDAC and Mnk are highly expressed in a variety of tumors; thus simultaneous inhibit HDAC and Mnk can increase the inhibitio…
View article: A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects
A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects Open
View article: Structure-Based Design of Novel Benzimidazole Derivatives as Pin1 Inhibitors
Structure-Based Design of Novel Benzimidazole Derivatives as Pin1 Inhibitors Open
Peptidyl-prolyl cis/trans isomerase Pin1 plays a key role in amplifying and translating multiple oncogenic signaling pathways during oncogenesis. The blockade of Pin1 provided a unique way of disrupting multiple oncogenic pathways and indu…
View article: Efficacité des pratiques en matière d’hygiène des mains dans la prévention de l’infection par le virus de la grippe en milieu communautaire : examen systématique
Efficacité des pratiques en matière d’hygiène des mains dans la prévention de l’infection par le virus de la grippe en milieu communautaire : examen systématique Open
View article: Design, synthesis and biological evaluation of benzimidazole derivatives as novel human Pin1 inhibitors
Design, synthesis and biological evaluation of benzimidazole derivatives as novel human Pin1 inhibitors Open
View article: Design, synthesis and biological evaluation of ring A modified 11-keto-boswellic acid derivatives as Pin1 inhibitors with remarkable anti-prostate cancer activity
Design, synthesis and biological evaluation of ring A modified 11-keto-boswellic acid derivatives as Pin1 inhibitors with remarkable anti-prostate cancer activity Open
View article: HDAC and Ku70 axis- an effective target for apoptosis induction by a new 2-cyano-3-oxo-1,9-dien glycyrrhetinic acid analogue
HDAC and Ku70 axis- an effective target for apoptosis induction by a new 2-cyano-3-oxo-1,9-dien glycyrrhetinic acid analogue Open
Methyl 2-cyano-3,12-dioxo-18β-olean-1,9(11)-dien-30-oate (CDODO-Me, 10d) derived from glycyrrhetinic acid and methyl-2-cyano-3,12-dioxooleana-1,9-dien-28-oic acid (CDDO-Me) derived from oleanoic acid are potent apoptosis inducers developed…
View article: Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif Open
View article: Conjugates of 18β-glycyrrhetinic acid derivatives with 3-(1H-benzo[d]imidazol-2-yl)propanoic acid as Pin1 inhibitors displaying anti-prostate cancer ability
Conjugates of 18β-glycyrrhetinic acid derivatives with 3-(1H-benzo[d]imidazol-2-yl)propanoic acid as Pin1 inhibitors displaying anti-prostate cancer ability Open
View article: Design and synthesis of novel 2-substituted 11-keto-boswellic acid heterocyclic derivatives as anti-prostate cancer agents with Pin1 inhibition ability
Design and synthesis of novel 2-substituted 11-keto-boswellic acid heterocyclic derivatives as anti-prostate cancer agents with Pin1 inhibition ability Open
View article: Synthesis and biological evaluation of quinoline derivatives as potential anti-prostate cancer agents and Pim-1 kinase inhibitors
Synthesis and biological evaluation of quinoline derivatives as potential anti-prostate cancer agents and Pim-1 kinase inhibitors Open
View article: Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy
Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy Open
View article: Design and synthesis of substituted pyrido[3,2-d]-1,2,3-triazines as potential Pim-1 inhibitors
Design and synthesis of substituted pyrido[3,2-d]-1,2,3-triazines as potential Pim-1 inhibitors Open
View article: Synthesis, biological evaluation and molecular modeling studies of psammaplin A and its analogs as potent histone deacetylases inhibitors and cytotoxic agents
Synthesis, biological evaluation and molecular modeling studies of psammaplin A and its analogs as potent histone deacetylases inhibitors and cytotoxic agents Open
View article: Novel thiol-based histone deacetylase inhibitors bearing 3-phenyl-1H-pyrazole-5-carboxamide scaffold as surface recognition motif: Design, synthesis and SAR study
Novel thiol-based histone deacetylase inhibitors bearing 3-phenyl-1H-pyrazole-5-carboxamide scaffold as surface recognition motif: Design, synthesis and SAR study Open
View article: Direct access to pyrido/pyrrolo[2,1-<i>b</i>]quinazolin-9(1<i>H</i>)-ones through silver-mediated intramolecular alkyne hydroamination reactions
Direct access to pyrido/pyrrolo[2,1-<i>b</i>]quinazolin-9(1<i>H</i>)-ones through silver-mediated intramolecular alkyne hydroamination reactions Open
We report a synthetic methodology for the construction of the fused heterocyclic compounds pyrido[2,1- b ]quinazolin-9(1 H )-ones and pyrrolo[2,1- b ]quinazolin-9(1 H )-ones through an AgOTf-catalyzed intramolecular alkyne hydroamination r…
View article: Dihydroartemisinin and its derivative induce apoptosis in acute myeloid leukemia through Noxa-mediated pathway requiring iron and endoperoxide moiety
Dihydroartemisinin and its derivative induce apoptosis in acute myeloid leukemia through Noxa-mediated pathway requiring iron and endoperoxide moiety Open
Anti-apoptotic protein Mcl-1 plays an important role in protecting cell from death in acute myeloid leukemia (AML). The apoptosis blocking activity of Mcl-1 is inhibited by BH3-only protein Noxa. We found that dihydroartemisinin (DHA) and …