Case report: Clinicopathological characteristic of two cases of primary endometrial squamous cell carcinoma and review of the literature.

Primary endometrial squamous cell carcinoma (PESCC) is a rare malignant tumor. To investigate the clinical and pathological features of PESCC, two cases of PESCC in Fujian Maternal and Child Health Hospital were retrospectively studied and the literatures were reviewed. Both of the two cases were menopausal women aged 57-62 years, clinically presenting with "vaginal discharge".

Binding and Assembly of a Benzotriazole Cavitand in Water.

A water-soluble cavitand bearing a benzotriazole upper rim was prepared and characterized. It exists as a dimeric velcraplex in D O, but forms host-guest complexes with hydrophobic and amphiphilic guests. Alkanes (C5 to C10), cyclic ketones (C6-C10), cyclic alcohols (C6-C8) and various amphiphilic guests form 1 : 1 cavitand complexes.

Hydrophobic and Metal-Coordinated Confinement Effects Trigger Recognition and Selectivity.

We report the synthesis and characterization of a new water-soluble cavitand . The container features 2-aminobenzimidazole panels at the "rim" and pyridiniums at the "feet". In the solid state, a single-crystal X-ray structure of the organic-soluble precursor showed a stable vase form.

Binding selectivity and separation of p-functionalized toluenes with a metallo-cavitand in water.

A metallo-cavitand (1-2Pd) showed unprecedented binding selectivity and sequestration of p-functionalized toluene isomers in water. The host-guest complexation was studied using 1H and COSY NMR methods and xylene-isomer complexes were examined by using DFT calculations. A liquid-liquid extraction scheme was developed for the separation of p-functionalized toluenes.

WZ66, a novel acetyl-CoA carboxylase inhibitor, alleviates nonalcoholic steatohepatitis (NASH) in mice.

The global prevalence of nonalcoholic steatohepatitis (NASH) increases incredibly. NASH ends up to advanced liver disease, which is highly threatening to human health. Currently, treatment of NASH is very limited.

Synthesis and anti-hepatocellular carcinoma activity of novel O-vinyl diazeniumdiolate-based nitric oxide-releasing derivatives of oleanolic acid.

Considering that high levels of nitric oxide (NO) exert anti-cancer effect and the derivatives of oleanolic acid (OA) have shown potent anti-cancer activity, new O-vinyl diazeniumdiolate-based NO releasing derivatives (5a-l, 11a-l) of OA were designed, synthesized, and biologically evaluated in the present study. These derivatives could release different amounts of NO in liver cells. Among them, 5d, 5i, 5j, 11g, 11h, and 11j released more NO in SMMC-7721 cells and displayed stronger proliferative inhibition against SMMC-7721 and HepG2 cells than OA and other tested compounds.

Synthesis and blocking activities of a new class of α₁-adrenoceptor antagonists.

Finding effective chemotherapeutic agents for clinical use is a long-lasting goal in medicinal chemistry. In this study, we report a new class of α₁-adrenoceptor (α₁-AR) antagonists. Specifically, we describe the synthesis and the blocking activities toward α₁-AR of 7-(2-hydroxypropoxy)-3,4-dihydroisoquinolin-1(2H)-one 1 and its structurally perturbed analogs 2-11 that were designed according to the principle of bioisosterism.

Synthesis and biological evaluation of sulfonylurea and thiourea derivatives substituted with benzenesulfonamide groups as potential hypoglycemic agents.

A novel class of sulfonylurea and thiourea derivatives substituted with benzenesulfonamide groups were designed and synthesized. The target compounds were assayed for the effects on the insulin release of isolated rat pancreatic islets and the glucose transport in adipocytes of rats. Some of them exhibited high potency.

[Synthesis and antibacterial activity of imidazothiadiazoles and heterocyclic-amine Mannich-base hydrochloride].

To optimize the synthetic method and antibacterial activity of fused heterocyclic thiadiazole compounds, cyclocondensation of 2-(4-methoxyphenyl)-5-amino-1,3,4-thiadiazole (2) with alpha-chloro-4-chloro acetophenone (3) resulted in a key intermediate (4), 6 -(4-chlorophenyl)-2-(4-methoxyphenyl)-imidazo-[2,1-b][1,3,4]thiadiazole, which was carried out an nucleophilic substitution with substituted piperazine to give the corresponding free bases of piperazine (5a-5c), then followed by Mannich reaction with heterocyclicamines and formaldehyde to yield the corresponding Mannich bases, (1a-11) as respective hydrochloride salts. The structures were confirmed by IR, 1H NMR, MS and elemental analysis and the antibacterial activities in vitro of fifteen newly synthesized compounds were also tested against Gram positive bacteria and Gram negative bacteria with the standard 2-fold agar dilution method. The antibacterial results showed that the introduction of a polar group resulted in the enhancement of antibacterial activity in vitro.

Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer.

Exploration for new MDR-modulator utilizing tetrahydroisoquinoline as scaffold disclosed 6,7-dimethoxy-1-(3,4-dimethoxy)benzyl-2-(N-n-octyl-N'-cyano)guanyl-1,2,3,4-tetrahydroisoquinoline (7) as a readily accessible medicinal lead. Compound 7 possessed potent MDR reversal activity in the range of the reference compound verapamil, and had not cardiovascular activity compared to verapamil.

Halomonas caseinilytica sp. nov., a halophilic bacterium isolated from a saline lake on the Qinghai-Tibet Plateau, China.

A halophilic, Gram-negative bacterial strain, designated AJ261T, which was isolated from a soil sample from a salt lake on the Qinghai-Tibet Plateau, was subjected to a polyphasic taxonomic study. The isolate grew optimally in the presence of 3-5 % NaCl and used various carbohydrates as sole carbon and energy sources. The genomic DNA G+C content was 63.

4-[2-(3,4-Dimethoxy-phenethyl-amino)prop-oxy]-2-methoxy-benzamide.

The title compound, C(21)H(28)N(2)O(5), has two intra-molecular N-H⋯O hydrogen bonds. Inter-molecular N-H⋯O hydrogen bonds [graph-set motif R(2) (2)(8)] give rise to a dimer. Weak N-H⋯N hydrogen bonds between neighboring dimers further extend the crystal structure, which exhibits an infinite chain motif.

Halomonas saccharevitans sp. nov., Halomonas arcis sp. nov. and Halomonas subterranea sp. nov., halophilic bacteria isolated from hypersaline environments of China.

Three strains of Gram-negative, aerobic, neutrophilic and halophilic bacteria were isolated from samples of a salt lake on the Qinghai-Tibet Plateau and a subterranean saline well in the Si-Chuan Basin of China. These isolates, designated AJ275(T), AJ282(T) and ZG16(T), were investigated using a polyphasic approach. Based on 16S rRNA gene sequence analysis, the isolates could be affiliated to the genus Halomonas.

[Synthesis and antibacterial activity of 3-(4-piperazin-1-yl-phenyl)-s-triazolo [3,4-b] [1,3,4] thiadiazole hydrochlorides].

To study the synthetic method and antibacterial activity of water-soluble fused heterocyclic compounds containing piperazine group, the nucleophilic substitution of 3-(4-chlorophenyl)-6-substituted-s-triazolo-[3, 4-b] [1, 3, 4] thiadiazoles (2a - n) with piperazine in the presence of phase transfer catalyst TBAI afforded 3-(4-piperazin-1-yl-phenyl)-6-substituted-s-triazolo [3, 4-b] [1, 3, 4] thiadiazole and then followed by acid treatment afforded 3-(4-piperazin-1-yl-phenyl)-6-substituted-s-triazolo [ 3, 4-b] [1, 3, 4] thiadiazole hydrochlorides (3a - n). Twenty-eight new compounds were synthesized and their structures were confirmed by IR, 1H NMR, MS and element analysis. The in vitro antibacterial activities of all newly synthesized compounds were tested against Gram positive bacteria and Gram negative bacteria with the standard 2-fold agar dilution method.

Halorubrum arcis sp. nov., an extremely halophilic archaeon isolated from a saline lake on the Qinghai-Tibet Plateau, China.

A Gram-negative, aerobic, neutrophilic and extremely halophilic archaeon (strain AJ201(T)), isolated from Ayakekum salt lake on the Qinghai-Tibet Plateau, was investigated by a polyphasic approach. The DNA G+C content of strain AJ201(T) was 65.7 mol%.

[Genetic analysis of the br gene in halophilic archaea isolated from Xingjiang region].

Some novel members of extremely halophilic Archaea, strain AJ11, AJ12 and AJ13, were isolated from Aularz Lake located in Altun Mountain National Nature Reserve of Xinjiang Uygur Autonomous Region in China. Partial DNA fragments encoding a bacteriorhodopsin (BR) as well as for 16S rRNA of isolated strains were amplified by PCR and their DNA sequences were determined subsequently. On the basis of homology and phylogenetic analysis about 16S rDNA, it was considered that the isolated strains formed a microbiological population are the members of genus Natrinema.

[Synthesis and antibacterial activity of 3-(4-amino-5-methyl-s-triazol-3-sulfanyl)-1-phenyl-propan-1-one O-(5-substituted phenyl-[1,3,4] oxadiazol-2-methyl)-oximes].

Aim: To study the synthetic method and antibacterial activity of amino-heterocyclic compounds coupled oxime-ether group.

Methods: The treatment of 4-amino-3-methyl-5-mercapto-s-triazole (3) with beta-chlorophenyl-propanone to form amino-s-triazole sulfanylphenyl-propanone (4) sequentially followed by oximation with hydroxyl-amine to produce the oximes (5) and etherification with various oxadiazole chloromethanes (6a - j) to yield the title compounds (1a - j). The in vitro antibacterial activities of all newly synthesized compounds were tested against Gram positive bacteria and Gram negative bacteria with the standard 2-fold agar dilution method.

[Synthesis and vascular relaxing activity of arecoline derivatives coupled with nitric oxide donors].

Aim: To search for potential anti-atherosclerosis drugs with vascular relaxation activity, a series of agonists of endothelial targets were designed and synthesized.

Methods: Coupling N-methyl-1,2, 3,6-tetrahydrapyridine ring system with 3,4-dibenzenesulfonyl-1,2,5-oxadiazole-2-oxide through esterification or amidation, a series of arecoline derivatives containing NO donors were designed and synthesised.

Results: A novel series of compounds structurally related to arecoline have been prepared, the proposed structures of eighteen new compounds were established by IR, 1H NMR, MS spectroscopy and elemental analysis.

[Synthesis and antibacterial activity of 3-(5-substituted phenyl-[1,3,4] oxadiazole-2-yl-methylenethio)-5-pyridin-3-yl-[1,2,4] triazole-4-yl-amines].

Aim: To study on synthesis and antibacterial activity evaluation of polyheterocycles.

Methods: The condensation of 4-amino-3-pyridin-3-yl-4H-[1,2,4] triazole-5-thiol with 2-chloromethyl-5-substituted phenyl-[1,3,4] oxadiazoles gave the corresponding title heterocycle amines, and the in vitro antibacterial activity was primarily evaluated by the method of cup-plate diffusion solution.

Results: Twelve novel compounds were synthesized, and their structures were confirmed by IR, 1H NMR, MS and element analysis.

[Synthesis and antibacterial activity of 2-(3-pyridyl)-5-([(5-aryl-1,3,4-oxadiazol-2-yl) methylene]thio)-1,3,4-oxadiazoles].

Aim: Studies on synthesis and antibacterial activity of new heterocycles.

Methods: The cyclocondensation of [(3-pyridyl)-1,3,4-oxadiazol-2-yl] thio acetic acid with various aroyl hydrazines in the presence of POCl3 and xylene gave the corresponding titled compounds, and the in vitro antibacterial activity was primarily evaluated by the method of cupplate diffusion solution.

Results: Sixteen novel titled compounds were synthesized, their structures were confirmed by IR, 1HNMR, MS and elemental analysis.

[Synthesis and vasorelaxant activities of benzopyran-4-one hydrazone derivatives].

Aim: In search of more potent, less toxic and selective potassium channel openers.

Methods: According to the structure-activity relationships of benzopyran compounds and the features of structures of aprikalim, dofetilide and nifekalant, twenty benzopyran-4-one hydrazone derivatives have been designed and synthesized from 4-cyanophenos through acetylation, Fries rearrangment, cyclization, hydrazone, substitution reaction and so on. The compounds were tested for their vasorelaxant activity in low (30 mmol.