Effect of silencing CITED1 gene to regulate PI3K/AKT pathway on the biological function of PTC cells and its mechanism.

This study aims to investigate the effect of silencing the CITED1 gene to regulate the PI3K/AKT pathway on the biological function of papillary thyroid carcinoma (PTC) cells and its mechanism of action. Human PTC cells SW1736 were divided into 4 groups: control group, siCITED1 group, LY294002 group and siCITED1+LY294002 group. CITED1 was silenced by transfection with siCITED1 plasmid. The PI3K/AKT pathway was inhibited by LY294002 (5 µmmol/L). Each group was determined for cell proliferation, apoptosis and invasion capabilities, as well as PI3K/AKT transcription and protein expression levels. CITED1 mRNA and protein levels in the siCITED1 group and the siCITED1+LY294002 group were significantly lower than those in the control group (P < 0.05), and the two levels were not significantly different between the LY294002 group and the control group (P > 0.05). Compared with the control group, the siCITED1 group showed remarkably lower proliferation and invasion capabilities, and remarkably higher apoptosis rate (P < 0.05). There was no significant difference in proliferation, apoptosis and invasion capabilities between the LY294002 group and the siCITED1+LY294002 group (P > 0.05), both of which had significantly lower proliferation and invasion capabilities but significantly higher apoptosis rate than the siCITED1 group (P < 0.05). PI3K and AKT protein levels in the siCITED1 group were significantly lower than those in the control group (P < 0.05). The PI3K and AKT protein levels in the LY294002 group and the siCITED1+LY294002 group were not significantly different (P > 0.05), and were significantly lower than those in the siCITED1 group (P < 0.05). In conclusion: CITED1 silence may inhibit the progression of PTC cells by inhibiting the PI3K/AKT pathway.

Overexpressed ZC3H13 suppresses papillary thyroid carcinoma growth through m6A modification-mediated IQGAP1 degradation.

PURPOSE: The purpose of this study was to clarify the effect of ZC3H13 on the growth of papillary thyroid carcinoma (PTC). METHODS: Firstly, we used qRT-PCR and Western blot to compare the difference in the expression of ZC3H13 between normal thyroid epithelial cells and PTC cell lines. Then, ZC3H13 overexpression/knockout thyroid cancer cells were constructed by lentivirus transfection, and the effects of overexpression of ZC3H13 on the proliferation, migration and invasion of PTC cells were detected by CCK8 and transwell experiments. Lastly, MeRIP-qPCR, RIP and o Actinomycin D were used to verify that ZC3H13 regulated the expression of downstream target gene IQGAP1 through m6A modification. RESULTS: ZC3H13 expression was decreased in PTC cell lines BCPAP, KTC-1, k1, HTH83, and TPC-1. Proliferation, invasion, and migration of PTC cells were inhibited by overexpressed ZC3H13 but increased by knockdown of ZC3H13. IQGAP1 expression was suppressed by ZC3H13 overexpression but enhanced by ZC3H13 knockdown. In ZC3H13-overexpressed PTC cells, the m6A level of IQGAP1 mRNA was increased, and the IQGAP1 mRNA expression was decreased with the increasing time of Actinomycin D treatment. YTHDF2 enriched more IQGAP1 mRNA than IgG and knockdown of YTHDF2 reversed the effect of ZC3H13 overexpression on IQGAP1 mRNA stability. The xenograft tumor experiment in nude mice confirmed that the overexpression of ZC3H13 inhibited tumor growth, while overexpression of IQGAP1 could reverse the inhibitory effect of ZC3H13 overexpression on tumor growth. CONCLUSION: ZC3H13 mediates IQGAP1 mRNA degradation by promoting m6A modification of IQGAP1 mRNA, this provides a prospective therapeutic target for PTC.

Synthesis of cyclic gem-dinitro compounds via radical nitration of 1,6-diynes with Fe(NO3)3·9H2O.

Cyclic gem-dinitro compounds were obtained via nitration of 1,6-diynes using Fe(NO3)3·9H2O as the nitrating agent. The reaction proceeds at room temperature using a cheap nitrating agent. A number of gem-dinitro cyclic compounds were obtained in moderate to good yields. The reaction offers an easy and convenient protocol to prepare gem-dinitro compounds, which are not easily obtained via the known procedures.

Base-Controlled Three Component Reactions of Amines, Elemental Sulfur, and Styrenes: Synthesis of Thioamides under Metal-Free Conditions.

Three component reactions of olefins, amines, and sulfur were studied. Thioamidation of styrenes is base-controlled, and 2-phenylethanethioamides and benzothioamides were obtained selectively in the presence of two different bases. This protocol offers a simple and efficient procedure for the synthesis of thioamides.

Palladium-Catalyzed Sequential Heteroarylation/Acylation Reactions of Iodobenzenes: Synthesis of Functionalized Benzo[ d]oxazoles.

We report an efficient palladium-catalyzed approach to the synthesis of benzoxazole derivatives via sequential heteroarylation/acylation reaction of iodobenzenes. Three readily available starting materials, iodobenzenes, anhydrides, and benzoxazoles, were smoothly coupled to form new C-C bonds at the ortho and ipso positions of the iodobenzenes to afford 2-heteroaryl-3-acylbenzene derivatives in good yields.

Copper(I)-Catalyzed N-O Bond Formation through Vinyl Nitrene Mediated Pathway under Mild Conditions.

Copper(I)-catalyzed N-O bond formation reactions through vinyl nitrene-mediated pathway were described. The reactions of N-alkoxylbenzamides and 2 H-azirines afforded α-amino oxime ethers in good to excellent yields at room temperature, which involved the cleavage of C-N and N-O bonds and the construction of new N-O and C-N bonds. It offers an efficient, regio- and stereoselective synthetic route for α-amino oxime ethers.

Rhodium-catalyzed triazole-directed C-H bond functionalization of arenes with diazo compounds.

Heterocyclic compounds bearing 1,2,3-triazole scaffolds have found wide application both in medicinal chemistry and materials science. In this paper, rhodium(iii)-catalyzed triazole-directed alkylation reactions of arenes using diazo compounds as the alkylating agents are described. A number of polysubstituted arenes were provided from easily available materials in good yields under mild conditions. The reactions proceed via triazole-directed ortho C-H bond activation and subsequent carbene insertion originating from diazo compounds.

Special role of JUN in papillary thyroid carcinoma based on bioinformatics analysis.

BACKGROUND: Papillary thyroid carcinoma (PTC) is the most common malignancy in thyroid tissue, and the number of patients with PTC has been increasing in recent years. Discovering the mechanism of PTC genesis and progression and finding new potential diagnostic biomarkers/therapeutic target genes of PTC are of great significance. METHODS: In this work, the datasets GSE3467 and GSE3678 were downloaded from the Gene Expression Omnibus (GEO) database. Differentially expressed genes (DEGs) were identified with the limma package in R. GO function and KEGG pathway enrichment were conducted with DAVID tool. The interaction network of the DEGs and other genes was performed with Cytoscape plugin BisoGenet, while clustering analysis was performed with Cytoscape plugin ClusterOne. RESULTS: A total of 1800 overlapped DEGs were detected in two datasets. Enrichment analysis of the DEGs found that the top three enriched GO terms in three ontologies and four significantly enriched KEGG pathways were mainly concerned with intercellular junction and extracellular matrix components. Interaction network analysis found that transcription factor hepatocyte nuclear factor 4, alpha (HNF4A) and DEG JUN had higher connection degrees. Clustering analysis indicated that two function modules, in which JUN was playing a central role, were highly relevant to PTC genesis and progression. CONCLUSIONS: JUN may be used as a specific diagnostic biomarker/therapeutic molecular target of PTC. However, further experiments are still needed to confirm our results.

Palladium-Catalyzed Sequential Acylation/Cyanation of Aryl Iodides: A Regiospecific Synthesis of 2-Cyanoaryl Ketones.

A palladium-catalyzed, norbornene-mediated acylation/cyanation reaction of iodobenzene was developed by the use of acyl chlorides as acylation reagents and cuprous cyanide. The reaction gave the 2-cyanoaryl ketones efficiently by using readily available starting materials.

Enhancement of N-heterocyclic carbenes on rhodium catalyzed olefination of triazoles.

A few rhodium complexes of N-heterocyclic carbenes were prepared through carbene transfer reactions and their structures were characterized by X-ray diffraction analysis. The rhodium complexes of NHCs are found to be efficient catalysts for vinylation of various triazoles via C-H activation. A number of double vinylated triazoles can be obtained in good yields.

Synthesis and structures of ruthenium-NHC complexes and their catalysis in hydrogen transfer reaction.

Ruthenium complexes [Ru(L1)2(CH3CN)2](PF6)2 (1), [RuL1(CH3CN)4](PF6)2 (2) and [RuL2(CH3CN)3](PF6)2 (3) (L1= 3-methyl-1-(pyrimidine-2-yl)imidazolylidene, L2 = 1,3-bis(pyridin-2-ylmethyl)benzimidazolylidene) were obtained through a transmetallation reaction of the corresponding nickel-NHC complexes with [Ru(p-cymene)2Cl2]2 in refluxing acetonitrile solution. The crystal structures of three complexes determined by X-ray analyses show that the central Ru(II) atoms are coordinated by pyrimidine- or pyridine-functionalized N-heterocyclic carbene and acetonitrile ligands displaying the typical octahedral geometry. The reaction of [RuL1(CH3CN)4](PF6)2 with triphenylphosphine and 1,10-phenanthroline resulted in the substitution of one and two coordinated acetonitrile ligands and afforded [RuL1(PPh3)(CH3CN)3](PF6)2 (4) and [RuL1(phen)(CH3CN)2](PF6)2 (5), respectively. The molecular structures of the complexes 4 and 5 were also studied by X-ray diffraction analysis. These ruthenium complexes have proven to be efficient catalysts for transfer hydrogenation of various ketones.

Copper-catalyzed cascade cyclization reaction of 2-haloaryltriazenes and sodium azide: selective synthesis of 2H-benzotriazoles in water.

A new approach to the synthesis of 2H-benzotriazoles is described. This strategy is based on the copper-catalyzed C-N coupling of 2-haloaryltriazenes or 2-haloazo compounds with sodium azide and the intramolecular addition of nitrene to N=N bonds. This approach allows the synthesis of various N-amino- and N-aryl-2H-benzotriazoles in water, in good to excellent yields. The procedure is simple and the starting materials and catalyst are easily available, offering a practical and convenient synthetic route to 2-substituted benzotriazoles.

N-heterocyclic carbene-stabilized palladium complexes as organometallic catalysts for bioorthogonal cross-coupling reactions.

A small library of water-soluble N-heterocyclic carbene (NHC)-stabilized palladium complexes was prepared and applied for cross-couplings of biomolecules under mild conditions in water. Pd-NHC complexes bearing hydrophilic groups were demonstrated to be efficient catalysts for the Suzuki-Miyaura coupling of various unnatural amino acids and proteins bearing p-iodophenyl functional groups. We further utilized this catalytic system for the rapid bioorthogonal labeling of proteins on the surfaces of mammalian cells. These results demonstrated that NHC-stabilized metal complexes have potential utility in cellular systems.

Di-, tri-, and tetranuclear copper(I) complexes of phenanthroline-linked dicarbene ligands.

A family of 2,9-di(3-R-1H-imidazolium-1-yl)-1,10-phenanthroline iodides and hexafluorophosphates (R = allyl, benzyl, mesityl, picolyl) were synthesized from 2,9-diiodophenanthroline and imidazole or N-substituted imidazoles. Simple reactions of these diimidazolium salts with copper powder at room temperature have afforded a series of multinuclear copper(I)-NHC complexes in good yields. The structures vary depending on the N substituents and counterions. [Cu4(L1)2(MeCN)4](PF6)4 (R = allyl) exhibits a zigzag Cu4 chain with two terminal [Cu(NHC)(MeCN)2] and two internal [Cu(phen)(NHC)] moieties. [Cu3(L2)2](PF6)3 (R = benzyl) contains a strictly linear Cu3 framework with two [Cu(NHC)2] units and a [Cu(phen)2] located at the center. Both complexes [Cu3(L4)2](PF6)3 (R = mesityl) and [Cu3(L5)2](PF6)3 (R = picolyl) consist of a triangular Cu3 core in which two copper(I) ions are surrounded by a phen and a NHC group and the third copper(I) is coordinated by two NHC groups. [Cu3(L3)2](PF6)3 derived from 2,9-di(3-benzyl-1H-benzimidazolium-1-yl)-1,10-phenanthroline hexafluorophosphate can undergo transannulation of the benzimidazolylidene ring giving [Cu2(L3')2](PF6)2. The decomposition process might involve solvent-induced rearrangement of the ligand and hydrolysis of carbene moieties. Treatment of 2,9-di(3-mesityl-1H-benzimidazolium-1-yl)-1,10-phenanthroline iodide with copper powder generated dinuclear complex [Cu2(L4)2][Cu2(µ-I)2I2] (R = mesityl) possessing a macrocyclic cation and [Cu2(µ-I)2I2](2-) anion. Tetranuclear complex [Cu4(L5)2(µ-I)2](CuI3) (R = picolyl) has been obtained from its diimidazolium iodide and copper powder. All Cu(I) complexes have been characterized by X-ray single diffraction analysis, elemental analysis, and NMR spectra. Their redox behavior and fluorescent properties have also been studied.

Pd/NHC catalyzed reduction and coupling of nitroaromatics for the synthesis of diarylamines.

Herein, we report a one-pot approach to diarylamines through the reductive homocoupling of nitroaromatics, employing triethylsilane as the reducing agent and Pd/NHC as the catalyst. This method enables nitroaromatics to serve both as electrophilic reagents and as precursors of nucleophilic reagents, allowing for the direct preparation of diarylamines without the need to isolate aromatic primary amines.

Cu-NHC-TEMPO catalyzed aerobic oxidation of primary alcohols to aldehydes.

Imidazolium salts bearing TEMPO groups react with commercially available copper powder affording Cu-NHC complexes. The in situ generated Cu-NHC-TEMPO complexes are quite efficient catalysts for aerobic oxidation of primary alcohols into aldehydes. The catalyst is easily available, and various primary alcohols were selectively converted to aldehydes in excellent yields.

Clinical efficacy of gasless submental-transoral endoscopic thyroidectomy with Kirschner wire suspension for papillary thyroid carcinoma.

PURPOSE: To analyze the clinical efficacy of gasless submental-transoral endoscopic thyroidectomy (ETE) with Kirschner wire suspension in patients with papillary thyroid carcinoma (PTC). METHODS: Retrospectively, we enrolled 112 patients with PTC who received treatment in The Second Affiliated Hospital of Nanchang University between December 2020 and December 2021. Among them, 60 cases (laparoscopic group) received gasless submental-transoral ETE with Kirschner wire suspension, and the other 52 cases (open group) were treated by traditional thyroidectomy. Surgical indicators (operative time (OT), intraoperative blood loss (IBL), and postoperative drainage volume (DV)), number of central lymph node (CLN) dissected, length of hospital stay (LOS), Visual Analogue Scale (VAS) score, aesthetic satisfaction score, and complications were observed and compared between the two groups. RESULTS: There was no significant difference between the two groups in OT (55.73±5.49 min vs. 55.00±7.79 min), IBL (20.67±7.75 mL vs. 23.08±6.24 mL), postoperative DV (33.17±15.09 mL vs. 39.52±19.22 mL), number of CLN dissected (5.54±2.75 vs. 5.43±3.15), LOS (3.63±0.69 d vs. 3.68±0.57 d), postoperative VAS score (3.19±1.07 points vs. 3.38±1.09 points), and total complication rate (3.85% vs. 8.33%; all P>0.05). However, the laparoscopic group exhibited a significantly higher aesthetic satisfaction score than the open group (7.10±1.46 points vs. 6.42±1.46 points; P<0.05). In addition, patients in both groups were followed up for at least 3 months, and no recurrence or metastasis was observed. CONCLUSIONS: Gasless submental-transoral ETE with Kirschner wire suspension offers comparable curative effect as traditional thyroidectomy and safety, but it provides superior esthetic results, making it a viable treatment option for patients with PTC.

Iron-catalyzed N-alkylation of azoles via cleavage of an sp3 C-H bond adjacent to a nitrogen atom.

Iron-catalyzed direct C-N bond formation between azoles and amides is described. The oxidative coupling reactions of sp(3) C-H bonds adjacent to a nitrogen atom in amides and sulfonamides with the N-H bond in azoles proceeded smoothly in the presence of FeCl(2) and di-tert-butyl peroxide (DTBP).

Construction of Heterobiaryl Skeletons through Pd-Catalyzed Cross-Coupling of Nitroarenes and Heterocyclic Arylborononate Esters with a Sterically Demanding NHC Ligand.

The palladium-catalyzed Suzuki-Miyaura cross-couplings of nitroarenes and heteroarylboronate esters has been developed. A number of heterobiaryl compounds containing pyridine, pyrimidine, quinoline, furan, thiophene, and pyrazole were prepared using [Pd(cinnamyl)Cl]2/2-aryl-5-(2,4,6-triisopropylphenyl)-2,3-imidazolylidene[1,5-a]pyridines as the catalysts in good to excellent yields. The synthetic practicality of this approach is demonstrated through the synthesis of druglike molecules.

Direct C-N coupling of imidazoles and benzylic compounds via iron-catalyzed oxidative activation of C-H bonds.

Iron-catalyzed direct C-N bond formation between imidazoles and benzylic hydrocarbons is described. The reaction utilizes an inexpensive iron catalyst-oxidant system that is suitable for the coupling of a range of benzylic C-H bonds with various imidazoles.