Brønsted Acid-Catalyzed Intramolecular Tandem Double Cyclization of γ-Hydroxy Acetylenic Ketones with Alkynes into Naphtho[1,2-]furan-3-ones.

A metal-free and atom-economic route for the synthesis of naphtho[1,2-]furan-3-ones has been realized via -TsOH·HO-catalyzed intramolecular tandem double cyclization of γ-hydroxy acetylenic ketones with alkynes in formic acid. The benzene-linked furanonyl-ynes are the key intermediates obtained by the scission/recombination of C-O double bonds. Further, the structural modifications of the representative product were implemented by reduction, demethylation, substitution, and [5 + 2]-cycloaddition.

Dual Proton/Silver-Catalyzed Serial (5 + 2)-Cycloaddition and Nazarov Cyclization of ()-2-Arylidene-3-hydroxyindanones with Conjugated Eneynes: Synthesis of Indanone-Fused Benzo[]azulenes.

A one-pot step-economic tandem process involving (5 + 2)-cycloaddition and Nazarov cyclization reactions has been reported for the facile synthesis of indanone-fused benzo[]azulenes from ()-2-arylidene-3-hydroxyindanones and conjugated eneynes. This highly regio- and stereoselective bisannulation reaction is enabled by dual silver and Brønsted acid catalysis and opens up a new avenue for the construction of important bicyclo[5.3.

Visible-Light-Mediated Tandem Difluoromethylation/Cyclization of Alkenyl Aldehydes toward CFH-Substituted Chroman-4-one Derivatives.

An efficient and facile visible-light-mediated tandem difluoromethylation/cyclization of alkenyl aldehydes, with easily accessible and air-stable [PhPCFH]Br as the difluoromethylation reagent, has been established. A range of CFH-substituted chroman-4-one skeletons and their derivatives, such as 2,3-dihydroquinolin-4(1)-ones, chroman, 3,4-dihydronaphthalen-1(2)-one, 2,3-dihydrobenzofuran, and 2,3-dihydro-1-inden-1-one, are efficiently produced in moderate to good yields with excellent chemoselectivity under mild reaction conditions.

[Effect of Netrin-1 on VEGFA Expression in T-ALL Cells and Its Related Mechanism].

Unlabelled: AbstractObjective: To investigate the effect of the axon guidance factor Netrin-1 on the expression of VEGFA in T cell acute lymphoblastic leukemia(T-ALL) and its related mechanism.

Methods: ELISA assays were applied to detect the levels of Netrin-1 and VEGFA in the bone marrow (BM) samples from children in the T-ALL and control group. The level of Netrin-1 and VEGFA were compared between control children and patients, and the liner correlation between Netrin-1 and VEGFA was analyzed.

Progress towards the Total Syntheses of Amaryllidaceae Alkaloids γ-Lycorane.

γ-Lycorane, a degradation product of the Aromaticaceae alkaloid lycorine, is one of the most attractive molecules in the Aromaticaceae family. It remains a popular target for synthesis due to its pentacyclic structure, which presents a vehicle for demonstrating the utility of new synthetic strategies. Various synthetic methods have been developed by synthetic chemists since the first synthesis of γ-lycorane by Nasuo in 1966.

Transition-metal-free three-component coupling approach to QUINAP derivatives.

The aluminum(III) triflate catalyzed three-component coupling reaction of alkynes, amines and phosphorylated aryl aldehydes to access phosphoryl quinoline derivatives has been developed. The reaction proceeds in a simple system without the use of transition metals, ligands or additives, thus making it attractive for the fast preparation of a variety of new potential N-P bidentate ligands.

Visible-light-mediated tandem phosphorylation/cyclization for the synthesis of phosphorylated oxindoles.

The visible-light-mediated tandem phosphorylation/cyclization of -arylacrylamides with H-phosphine oxides has been developed for the synthesis of phosphorylated oxindoles. This efficient and facile process was useful for the construction of a C-P bond and triggered the formation of a C-C bond with good compatibility with functional groups undermild reaction conditions.

Prognostic significance of measurable residual disease based on multiparameter flow cytometry in childhood acute myeloid leukemia.

Objectives: To study the prognostic value of measurable residual disease (MRD) for childhood acute myeloid leukemia (AML) by analyzing MRD-guided risk stratification therapy.

Methods: A total of 93 children with AML were prospectively enrolled in this study. Chemotherapy with the 2015-AML-03 regimen was completed according to the risk stratification determined by genetic abnormality at initial diagnosis and MRD and bone marrow cytology after induction therapy I.

[Bioinformatics Analysis and Verification of Acute B-Lymphocytic Leukemia in Children with Isolated Bone Marrow Relapse].

Objective: To analyze the hub genes affecting the solely bone marrow relapse of childish acute B-cell lymphoblastic leukemia (B-ALL).

Methods: The high-throughput RNA sequencing data were downloaded from TCGA database, the differentially expressed genes were screened by DESeq2 package of R, and the differentially expressed genes were grouped by GO function enrichment analysis and KEGG pathway enrichment analysis. Further, the data of STRING database and Cytoscape software were used to construct protein interaction network, screen hub genes and highly interaction protein sub network, perform GO and KEGG analysis of the hub genes and protein sub network respectively.

[Clinical features and prognosis of pediatric acute megakaryocytic leukemia].

Objective: To study the clinical features and prognosis of children with acute megakaryocytic leukemia (AMKL) and the clinical effect of acute myeloid leukemia 03 (AML03) regimen for the treatment of pediatric AMKL.

Methods: The clinical data were collected from 47 children with AMKL who were diagnosed from May 2011 to December 2019. The treatment outcomes and prognostic factors were analyzed.

[Expression of Netrin-1 in Patients with Acute Lymphoblastic Leukemia and Its Clinical Significance].

Objective: To investigate the correlation of the Netrin-1 expression level with the clinical characteristics in children with acute lymphoblastic leukemia (ALL) and to explore its possible regulatory mechanism.

Methods: ELISA was used to detect the expression level of Netrin-1 in peripheral blood serum from 48 child ALL patients (newly diagnosed, recurrent), and its relevance with clinical indicators was statistically analyzed. The blood serum samples from 27 children with non malignant hematological diseases were choosen as controls.

[E-cadherin Expression in Children with Acute Leukemia and Its Clinical Significance].

Objective: To investigate the correlation of E-cadherin expression level with the clinical characterastics in children with acute leukemia (AL), and to explore the possible regulatory mechanism.

Methods: Real-time quantitative RT-PCR was applied to detect the expression level of E-cadherin in bone marrow samples from 135 child patients diagnosed as AL, and its relevance with clinical indicators was statistically analyzed. The expression levels of E-cadherin, β-catenin, and Akt/p-Akt were detected by using Western blot.

[Effect of 4' -Hydroxywogonin on Proliferation and Apoptosis of Human Acute Lymphoblastic Leukemia Cells].

Objective: To investigate the effect of 4' -hydroxywogonin on proliferation and apoptosis of human acute lymphoblastic leukemia SUP-B15 and Jurkat cells, and to analyze its possible mechanism.

Methods: SUP-B15 and Jurkat cells were cultivated in vitro and treated with different concentrations of 4' -hydroxywogonin, the inhibitory effect of 4' -hydroxywogonin on the proliferation of SUP-B15 and Jurkat cells was detected by CCK-8 method; the cell apoptosis was examined by the flow cytometry with Annexin V-APC/7-AAD donble staining; the expression of C-MYC, BCL-2 and cleaved caspase 3 in SUP-B15 and Jurkat cells were measured with Western blot.

Results: 4' -hydroxywogonin inhibited the proliferation of SUP-B15 and Jurkat cells in a dose-dependent manner (r=0.

[Expression of β-integrin family members in children with T-cell acute lymphoblastic leukemia].

Objective: To study the expression of β-integrin family members in children with T-cell acute lymphoblastic leukemia (T-ALL) and their significance.

Methods: Quantitative real-time PCR analyses were performed to assess the expression levels of β-integrin family members in bone marrow samples from 22 children with newly-diagnosed T-ALL and 21 controls (16 children with non-malignant hematologic disease and 5 healthy donors with bone marrow transplantation). Jurkat cells were treated with integrin inhibitor arginine-glycine-aspartate (Arg-Gly-Asp, RGD) peptide.

[PRPS1 Expression in Children with Acute Leukemia and Its Clinical Significance].

Objective: To investigate the correlation between the expression level of PRPS1 and the clinical characteristics in children with acute leukemia(AL).

Methods: Real-time quantitative RT-PCR and Western blot were used to detect the level of PRPS1 mRNA and protein expression in bone marrow samples from 176 patients diagnosed as AL (126 cases were newly diagnosed and 50 cases in complete remission), and its relevance with clinical indicators was statistically analyzed. The bone marrow samples from 21 children with non-malignant hematological disease were used as controls.

SIRT4 accelerates Ang II-induced pathological cardiac hypertrophy by inhibiting manganese superoxide dismutase activity.

Aims: Oxidative stress contributes to the development of cardiac hypertrophy and heart failure. One of the mitochondrial sirtuins, Sirt4, is highly expressed in the heart, but its function remains unknown. The aim of the present study was to investigate the role of Sirt4 in the pathogenesis of pathological cardiac hypertrophy and the molecular mechanism by which Sirt4 regulates mitochondrial oxidative stress.

Netrin-1 suppresses the MEK/ERK pathway and ITGB4 in pancreatic cancer.

The axon guidance factor netrin-1 promotes tumorigenesis in multiple types of cancers, particularly at their advanced stages. Here, we investigate whether netrin-1 is involved in the in vivo growth of pancreatic adenocarcinoma. We show that netrin-1 is significantly under-expressed in stage-I/II pancreatic ductal adenocarcinoma (PDAC).

A unique copper-catalyzed cross-coupling reaction by hydrogen (H2) removal for the stereoselective synthesis of 3-phosphoindoles.

The first Cu(i)-catalyzed cross-coupling reaction by hydrogen (H2) removal for the stereoselective synthesis of 3-phosphoindoles is reported. Going beyond the oxidative dehydrogenative coupling reactions reported recently, this reaction completely omits the oxidant and base, producing hydrogen (H2) as the only byproduct.

Regio- and stereoselective allylic C-H arylation with electron-deficient arenes by 1,1'-bi-2-naphthol-palladium cooperation.

A palladium-catalyzed allylic C-H arylation reaction with electron-deficient arenes with high regio- and stereoselectivity is reported. This work represents the first successful use of 1,1'-bi-2-naphthol as the ancillary ligand in allylic C-H activation, which is the key factor for chemoselectivity. Furthermore, high selectivity allylic C-H acetoxylation and amination were also successfully achieved under the same catalytic system.

Overexpression of mitofilin in the mouse heart promotes cardiac hypertrophy in response to hypertrophic stimuli.

Aims: Mitofilin was originally described as a heart muscle protein because of its abundance in the heart tissue; however, its function in the heart is still to be elucidated. Thus, this study aims at investigating the role of mitofilin in the heart in response to hypertrophic stimuli.

Results: In this study, a significant increase in mitofilin expression was observed in the hearts of patients with hypertrophic cardiomyopathy.

Pd(II)-catalyzed Ph2(O)P-directed C-H olefination toward phosphine-alkene ligands.

The Pd(II)-catalyzed Ph2(O)P-directed C-H olefination to synthesize alkene-phosphine compounds is reported. In contrast to previous examples of various directing groups that guide selective C-H activation, the Ph2(O)P group not only acts as the directing group but also serves to construct the alkene-phosphine ligands. The monoprotected amino acid (MPAA) ligand Ac-Leu-OH is found to promote this reaction in a significant manner.

Palladium-catalyzed sp2 and sp3 C-H bond activation and addition to isatin toward 3-hydroxy-2-oxindoles.

The first Pd(II)-catalyzed C-H addition to isatins by direct sp(2)/sp(3) C-H bond activation for the construction of 3-substituted-3-hydroxy-2-oxindoles is reported. The bidentate nitrogen ligands were found to promote this reaction. Specifically, the preliminary bioassay indicated that 3-(5-chlorobenzoxazole)-3-hydroxy-N-benzyl-2-oxindole (2w) is a new inhibitor of human kidney cancer and hepatocellular carcinoma cells.

Silver-catalyzed carboazidation of arylacrylamides.

A novel and inexpensive method of nontoxic, silver-salt-catalyzed carboazidation of arylacrylamides to afford corresponding azide oxindoles is reported. This reaction system exhibits great functional group tolerance. All products form a crucial skeleton for the synthesis of various indole alkaloids.

Palladium-catalyzed divergent reactions of 1,6-enyne carbonates: synthesis of vinylidenepyridines and vinylidenepyrrolidines.

A method for preparing five- or six-membered heterocyclic compounds from enyne carbonates via palladium catalysis was developed. Enyne carbonates were transformed into 3-vinylidene-1-tosylpyridines 2 in the presence of PdI(2) as the catalyst. Using Pd(dba)(2) as the catalyst, 3-vinylidene-1-tosylpyrrolidines 3 were obtained.