miR-93-5p suppresses ovarian cancer malignancy and negatively regulate CCND2 by binding to its 3'UTR region.

Ovarian cancer is the most fatal gynecological cancer worldwide, yet the fundamental mechanism of malignancy acquisition in ovarian cancer remains unknown. miRNA has been implicated to a variety of diseases, including cancer initiation and progression. Cyclin-D2 (CCND2) is ubiquitously implicated in cancer uncontrol cell proliferation. Bioinformatic research revealed that CCND2 is a candidate gene for miR-93-5p with a binding site in its 3'UTR region in the current study. Using our ovarian cancer sample, we verified that miR-93-5p is negatively correlated with CCND2 mRNA and protein levels. Luciferase report assay revealed miR-93-5p inhibits CCND2 production through binding to the 3'UTR region. The expression of miR-93-5p in ovarian cancer patient samples was then determined, and a survival analysis was performed. Our findings showed that miR-93-5p is downregulated in ovarian cancer and is a favorable predictive factor in ovarian cancer patient. CCK8 assay, wound healing assay and flow cytometry-based cell cycle and apoptotic cell analyses were employed here. We found that miR-93-5p suppresses ovarian cancer cell proliferation and migration while enhances cell death. Our research certified that miR-93-5p reduces ovarian cancer malignancy by targeting CCND2.

Focal adhesion kinase inhibitors, a heavy punch to cancer.

Kinases are the ideal druggable targets for diseases and especially were highlighted on cancer therapy. Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase and its aberrant signaling extensively implicates in the progression of most cancer types, involving in cancer cell growth, adhesion, migration, and tumor microenvironment (TME) remodeling. FAK is commonly overexpressed and activated in a variety of cancers and plays as a targetable kinase in cancer therapy. FAK inhibitors already exhibited promising performance in preclinical and early-stage clinical trials. Moreover, substantial evidence has implied that targeting FAK is more effective in combination strategy, thereby reversing the failure of chemotherapies or targeted therapies in solid tumors. In the current review, we summarized the drug development progress, chemotherapy strategy, and perspective view for FAK inhibitors.

Comparison of open reduction internal fixation and conservative treatment plus open reduction internal fixation for calcaneal fractures.

To compare the effect of open reduction internal fixation and conservative treatment combined with open reduction internal fixation for subjects with calcaneal fractures, 130 patients with calcaneal fractures were divided into observation group and control group. Observation group were treated with open reduction internal fixation and conservative treatment, control group treated as open reduction internal fixation. The healing related indicators, daily life activities ability score of observation group after treatment 6 months were significantly higher than that of the control group, there was no significant difference for the healing rate of excellent and good rate, the daily life activities ability score after one and three year between two groups. Open reduction internal fixation combined with conservative treatment in treatment of calcaneal fractures can clear anatomic structure and have fast function recovery. Thus, it should be as the preferred method for the treatment of calcaneal fractures.

Energetic N,N,N',N'-tetraaminopiperazinium salts.

The formation of terraminopiperazinium salts using water as solvent provides a green, straightforward approach to highly energetic salts that exhibit good thermal stabilities and moderate densities. The N,N,N',N'-tetraaminopiperazinium cation was selected for this study because of its high nitrogen-nitrogen bond content and its hign positive near or formation. Theoretical and empirical calculations on energetic salts based on this nitrogen-rich cation reveal them to have high positive molar enthalpies of formation, as high as 1034.0 kJ mol(-1), supporting the application of these new salts as potential energetic materials.

The synthesis of di(aminoguanidine) 5-nitroiminotetrazolate: some diprotic or monoprotic acids as precursors of energetic salts.

Syntheses of salts with 4,6-bis(nitroimino)-1,3,5-triazinan-2-one (DNAM), 3,5-dinitro-1,2,4-cyclopentanetrione (DDCP), 3-nitroiminotriazolate, and 5-nitroiminotetrazolate as anions yielded moderately dense nitro-containing energetic salts that are thermally stable to >200 degrees C (measured by thermogravimetric analysis). Di(aminoguanidine) 5-nitroiminotetrazolate (8) crystallizes in the monoclinic space group P2(1)/c with an essentially planar 5-nitroiminotetrazolate dianion. Based on experimental and calculated densities, and theoretical calculations carried out by using the Gaussian 03 suite of programs, all of the salts have calculated detonation pressures and velocities that exceed those of 2,4,6-trinitrotoluene (TNT) and a few have values that approach those of triaminotrinitrobenzene (TATB).

Synthesis of pentafluorosulfanylpyrazole and pentafluorosulfanyl-1,2,3-triazole and their derivatives as energetic materials by click chemistry.

1-Pentafluorosulfanyl acetylene and its derivatives react with azide or diazomethane giving rise to an SF5-substituted 1,2,3-triazole or pyrazole. The SF5 group increases density remarkably and as a result enhances the detonation performance of the energetic materials relative to the CF3 group.

2,4,5-trinitroimidazole-based energetic salts.

2,4,5-Trinitroimidazolate (TNI) salts with "high-nitrogen" cations tend to be highly hydrogen bonded and have heats of formation ranging up to 616 kJ mol(-1). Density, oxygen balance, and thermostability are enhanced by the presence of TNI. Based on theoretical calculations, all of the new salts are potential propellants.

Rapid and accurate estimation of densities of room-temperature ionic liquids and salts.

Volume parameters for room-temperature ionic liquids (RTILs) and salts were developed. For 59 of the most common imidazolium, pyridinium, pyrrolidinium, tetralkylammonium, and phosphonium-based RTILs, the mean absolute deviation (MAD) of the densities is 0.007 g cm-3; for 35 imidazolium-based room-temperature salts, the MAD is 0.020 g cm-3; and for 150 energetic salts, the MAD is 0.035 g cm-3. The experimental density (Y) for an alkylated imidazolium or pyridinium-based room-temperature ionic liquid is approximately proportional to its calculated density (X) in the solid state: Y = 0.948X - 0.110 (correlation coefficient: R2 = 0.998, for BF4-, PF6-, NTf2- -containing ionic liquids); Y = 0.934X - 0.070 (correlation coefficient: R2 = 0.999, for OTf-, CF3CO2-, N(CN)2- -containing ionic liquids).

Heterocyclic-based nitrodicyanomethanide and dinitrocyanomethanide salts: a family of new energetic ionic liquids.

Twelve novel energetic salts 1a-f and 2a-f with nitrodicyanomethanide and dinitrocyanomethanide anions paired with 1,5-diamino-4-methyltetrazolium, 1,4-dimethyl-5-aminotetrazolium 1,4,5-trimethyltetrazolium, 1-methyl-4-amino-1,2,4-triazolium, 1,4-dimethyltriazolium, and 1,3-dimethylimidazolium have been prepared through metathesis reactions of equivalent silver(I) salts with corresponding iodide salts in acetonitrile. Key physical properties, such as melting point, thermal stability and density, were measured. The relationship between their structures and these properties was determined. The structures of 1,5-diamino-4-methyltetrazolium-based salts 1a and 2a were further confirmed by single-crystal X-ray analysis. The densities and standard enthalpies of formation for these energetic salts were calculated. All of the salts possess higher enthalpies of formation than the nitrate analogues.

Energetic bicyclic azolium salts.

Bicyclic azoles, 2-methyl-5-(imidazol-1-yl)-2H-tetrazole (1), 2-methyl-5-(1,2,4-triazol-1-yl)-2H-tetrazole (4), 1-methyl-5-(imidazol-1-yl)-1H-tetrazole (7), 1-methyl-5-(1,2,4-triazol-1-yl)-1H-tetrazole (10), 1-methyl-4-nitro-2-(imidazol-1-yl)-1H-imidazole (13), and 1-methyl-4-nitro-2-(1,2,4-triazol-1-yl)-1H-imidazole (16) were prepared. Their thermally stable azolium salts, 3, 6, 9, 12, 15, and 18-21, with densities ranging between 1.519-1.674 g cm-3, were synthesized by quaternization with nitric or perchloric acid or with iodomethane followed by metathesis reactions with silver nitrate and silver perchlorate. The structures of 12 b and 21 b were confirmed by single-crystal X-ray analysis. The standard enthalpies of formation for some of the new salts were calculated by using the computationally feasible DFT(B3LYP) and MP2 methods in conjunction with an empirical approach based on densities of salts. The calculated values range from DeltaHdegreef=209.9 (21 a) to 412.3 (12 b) kJ mol-1 in which the experimental densities are >1.515 g cm-3.

Straightforward syntheses of hypervalent iodine(III) reagents mediated by Selectfluor.

Use of Selectfluor allows hypervalent iodine(III) species such as aryl iodine(III) difluoride, diacetate, and di(trifluoroacetate) and Koser's salt to be easily prepared. Aryl iodine(III) difluoride and diacetate can be synthesized from the corresponding arene and elemental iodine in one-pot procedures. [reaction: see text]

Bipyridinium ionic liquid-promoted cross-coupling reactions between perfluoroalkyl or pentafluorophenyl halides and aryl iodides.

A new room-temperature ionic liquid has been synthesized from 2,2'-bipyridine. This liquid improved the copper-catalyzed cross-coupling reactions between perfluoroalkyl or pentafluorophenyl halides and aryl iodides. Good recyclability using this solvent system was observed.

Energetic salts of azotetrazolate, iminobis(5-tetrazolate) and 5, 5'-bis(tetrazolate).

Energetic ionic salts of azotetrazolate (AT), iminobis(5-tetrazolate) (IBT) and 5, 5'-bis(tetrazole) (BT) were synthesized; 1-methyl-4-aminotriazolium azotetrazolate has a layered structure and exhibits a heat of formation of +4360 kJ kg(-1).

Structure-dependent oxidative bromination of unsaturated C-C bonds mediated by selectfluor.

A number of olefins were subjected to oxidative bromination using Selectfluor/KBr. For different types of substrates, addition, monobromine-substituted, or Hunsdiecker-Borodin reaction products can be readily afforded.

Syntheses of very dense halogenated liquids.

A family of halogenated liquids with densities ranging from 1.95 to 2.80 g cm(-3) was readily synthesized by a one-pot procedure. These liquids exhibit characteristics of ionic liquids with melting/transition points lower than room temperature, long liquid ranges, and marked hydrolytic and thermal stabilities.

A facile asymmetric route to (-)-aphanorphine.

8O-methylaphanorphine was synthesized from 4-methoxyphenylacetaldehyde in 36% overall yield and in nine steps, featuring the formation of ring B via a Friedel-Crafts alkylative cyclization with the concomitant stereospecific introduction of the benzylic quaternary carbon center. The current work constitutes an efficient enantioselective formal synthesis of 3-benzazepine marine alkaloid (-)-aphanorphine.