Tuning vibration-induced emission through macrocyclization and catenation.

In order to investigate the effect of macrocyclization and catenation on the regulation of vibration-induced emission (VIE), the typical VIE luminogen 9,14-diphenyl-9,14-dihydrodibenzo[a, c]phenazine (DPAC) was introduced into the skeleton of a macrocycle and corresponding [2]catenane to evaluate their dynamic relaxation processes. As investigated in detail by femtosecond transient absorption (TA) spectra, the resultant VIE systems revealed precisely tunable emissions upon changing the solvent viscosity, highlighting the key effect of the formation of [2]catenane. Notably, the introduction of an additional pillar[5]arene macrocycle featuring unique planar chirality endows the resultant chiral VIE-active [2]catenane with attractive circularly polarized luminescence in different states.

Extended phenothiazines: synthesis, photophysical and redox properties, and efficient photocatalytic oxidative coupling of amines.

Herein we successfully developed a ring-fusion approach to extend the conjugation length of phenothiazines and synthesized a series of novel extended phenothiazines 1-5. The intriguing π-conjugation length-dependent photophysical and redox properties of 1-5, and their photocatalytic performance towards visible-light-driven oxidative coupling reactions of amines were systematically investigated. The results indicated that this series of extended phenothiazines exhibited continuous red shifts of light absorption with increasing numbers of fused rings.

Synthesis and antitumour evaluation of indole-2-carboxamides against paediatric brain cancer cells.

Paediatric glioblastomas are rapidly growing, devastating brain neoplasms with an invasive phenotype. Radiotherapy and chemotherapy, which are the current therapeutic adjuvant to surgical resection, are still associated with various toxicity profiles and only marginally improve the course of the disease and life expectancy. A considerable body of evidence supports the antitumour and apoptotic effects of certain cannabinoids, such as WIN55,212-2, against a wide spectrum of cancer cells, including gliomas.

Recent advances and perspectives on supramolecular radical cages.

Supramolecular radical chemistry has been emerging as a cutting-edge interdisciplinary field of traditional supramolecular chemistry and radical chemistry in recent years. The purpose of such a fundamental research field is to combine traditional supramolecular chemistry and radical chemistry together, and take the benefit of both to eventually create new molecules and materials. Recently, supramolecular radical cages have been becoming one of the most frontier and challenging research focuses in the field of supramolecular chemistry.

Palladium/Xu-Phos-catalyzed asymmetric carboamination towards isoxazolidines and pyrrolidines.

An efficient palladium-catalyzed enantioselective carboamination reaction of -Boc--homoallyl-hydroxylamines and -Boc-pent-4-enylamines with aryl or alkenyl bromides was developed, delivering various substituted isoxazolidines and pyrrolidines in good yields with up to 97% ee. The reaction features mild conditions, general substrate scope and scalability. The obtained products can be transformed into chiral 1,3-aminoalcohol derivatives without erosion of chirality.

Construction of polycyclic structures with vicinal all-carbon quaternary stereocenters an enantioselective photoenolization/Diels-Alder reaction.

All-carbon quaternary stereocenters are ubiquitous in natural products and significant in drug molecules. However, construction of all-carbon stereocenters is a challenging project due to their congested chemical environment. And, when vicinal all-carbon quaternary stereocenters are present in one molecule, they will dramatically increase its synthetic challenge.

Hierarchical self-assembly of discrete bis-[2]pseudorotaxane metallacycle with bis-pillar[5]arene host-guest interactions and their redox-responsive behaviors.

A discrete rhomboidal metallacycle R functionalized with bis-[2]pseudorotaxane of [Cu(phenanthroline)] derivatives was successfully synthesized coordination-driven self-assembly. Furthermore, the host-guest complexation of such a bis-[2]pseudorotaxane metallacycle with a bis-pillar[5]arene (bisP5) allowed for the formation of a new family of cross-linked supramolecular polymers R⊃(bisP5), which displayed interesting redox-responsive properties. By taking advantage of the substantial structural differences between the coordination geometries of [Cu(phenanthroline)] and [Cu(phenanthroline)], the weight-average diffusion coefficients of the supramolecular polymer were adjusted through changing the redox state of the Cu(i)/Cu(ii) complexes.

A neutral Cu-based MOF for effective quercetin extraction and conversion from natural onion juice.

We report herein a new microporous neutral three-dimensional (3D) metal-organic framework [Cu(L)(DMF)(HO)]· (1·) composed of copper paddle-wheel and flexible tetracarboxylic acid linkers (DMF = ,-dimethylformamide, HL = tetrakis[(6-carboxynaphthoxy)methyl]methane). Surprisingly, this MOF with neutral cavities can not only extract pure quercetin (QT) but also convert it into Cu-QT during the desorption process. It has been well characterized by UV-vis, IR, ESI-MS and TEM-EDS studies.

One-step preparation of N,O co-doped 3D hierarchically porous carbon derived from soybean dregs for high-performance supercapacitors.

Hierarchically porous carbon (HPC) material based on environmental friendliness biomass has spurred much attention, due to its high surface area and porous structure. Herein, three-dimensional (3D) N,O co-doped HPC (N-O-HPC) was prepared by using a one-step fabrication process of simultaneously carbonizing and activating soybean dregs and used as an electrode for supercapacitors (SCs). The obtained N-O-HPC with 4.

Discovery of methylpyrimidine ring-fused diterpenoid analogs as a novel testosterone synthesis promoter.

Herein we screened our small synthetic library of diterpenoid analogs for hit compounds on promoting testosterone synthesis and the methylpyrimidine ring-fused diterpenoid analog 7 was obtained as the hit. Based on the hit, a series of derivatives were designed, synthesized and evaluated for their effects on testosterone secretion in mouse Leydig TM3 cells. Most of the derivatives showed better activity in promoting testosterone synthesis than the positive control compound icariin, among which compound 17 has optimal activity and little cytotoxicity.

Cross-linked poly(ionic liquid) as precursors for nitrogen-doped porous carbons.

A soluble and easily dispersive cross-linked poly(ionic liquid), copolymer of 1-vinyl-3-butylimidazolium bromide ([VBIM][Br]) and divinylbenzene (DVB), was used as a precursor for nitrogen doped porous carbons (NPCs) with SiO (from tetraethyl orthosilicate) as a template. The NPCs were characterized by infrared (IR) spectroscopy, nitrogen adsorption-desorption, scanning electron microscopy (SEM), transmission electron microscopy (TEM), X-ray diffraction (XRD), Raman spectroscopy, thermo gravimetric analysis (TGA), elemental analysis and X-ray photoelectron spectroscopy (XPS). The specific surface area and porosity of NPCs depended on the carbonization temperature, the SiO/[VBIM][Br] ratio and the precursors.

Efficient and Recyclable RuCl ⋅ 3HO Catalyst Modified with Ionic Diphosphine for the Alkoxycarbonylation of Aryl Halides.

A series of ionic (mono-/di-)phosphines (, , and ) with structural similarity and their corresponding neutral counterparts (, , and ) were applied to modulate the catalytic performance of RuCl ⋅ 3HO. With the involvement of the ionic diphosphine (), in which the two phosphino-fragments were linked by butylene group, RuCl ⋅ 3HO with advantages of low cost, robustness, and good availability was found to be an efficient and recyclable catalyst for the alkoxycarbonylation of aryl halides. The -based RuCl ⋅ 3HO system corresponded to the best conversion of PhI (96 %) along with 99 % selectivity to the target product of methyl benzoate as well as the good generality to alkoxycarbonylation of different aryl halides (ArX, X=I and Br) with alcohols MeOH, EtOH, -PrOH and -BuOH.

At room temperature in water: efficient hydrogenation of furfural to furfuryl alcohol with a Pt/SiC-C catalyst.

Selective hydrogenation of furfural (FAL) to furfuryl alcohol (FOL) is challenging because of many side reactions. The highly selective hydrogenation of FAL to FOL can be achieved over a Pt catalyst supported on nanoporous SiC-C composites even at room temperature in water. A Pt/SiC-C-200-H catalyst, which had a Pt loading of 3 wt% and was reduced in flowing hydrogen at 500 °C after calcination in air at 200 °C for 2 h, furnished complete FAL conversion and over 99% selectivity to FOL at 25 °C under 1 MPa of hydrogen in water.

Discovery of -cyclobutylaminoethoxyisoxazole derivatives as novel sigma-1 receptor ligands with neurite outgrowth efficacy in cells.

Herein we reported a series of 14 novel derivatives based on the -cyclobutylaminoethoxyisoxazole scaffold. binding studies of these compounds demonstrated their low nanomolar to subnanomolar potencies as σ1 receptor ligands, with moderate to excellent selectivity over the σ2 receptor as represented by compounds 17-30. The majority of the derivatives scored high (>4.

Maleimidation of dextran and the application in designing a dextran-camptothecin conjugate.

Camptothecin analogs, as commonly used chemotherapy drugs, usually have poor water solubility which has limited their use in the clinic. In order to improve the water-solubility of camptothecin, a new dextran derivative Dex-Mal was synthesized and used in designing a dextran-camptothecin conjugate which contained a CTB-sensitive linker. This conjugate could efficiently release the therapeutic drug SN-38 in the presence of cathepsin B and the antiproliferative activity of the conjugate was similar to the approved drug Irinotecan hydrochloride.

Novel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors.

Herein we describe the design, synthesis, and biological evaluation of a novel series of tranylcypromine-based LSD1 inhibitors conformational restriction using spiro ring systems. A simple, direct spirocyclic analog of tranylcypromine (compounds 8a and 8b) was shown to be a 28- to 129-fold more potent inhibitor of LSD1 enzyme compared to tranylcypromine. Further incorporation of various substituted benzyl groups to the amino group resulted in a suite of 2',3'-dihydrospiro[cyclopropane-1,1'-inden]-2-amines that are potent LSD1 inhibitors with excellent selectivity profiles (14a, 15b, 16a, 19a and 20b) against closely related enzymes such as MAO-A, MAO-B, and LSD2.

The potent and selective α4β2*/α6*-nicotinic acetylcholine receptor partial agonist 2-[5-[5-((S)Azetidin-2-ylmethoxy)-3-pyridinyl]-3-isoxazolyl]ethanol demonstrates antidepressive-like behavior in animal models and a favorable ADME-tox profile.

Preclinical and clinical studies demonstrated that the inhibition of cholinergic supersensitivity through nicotinic antagonists and partial agonists can be used successfully to treat depressed patients, especially those who are poor responders to selective serotonin reuptake inhibitors (SSRIs). In our effort to develop novel antidepressant drugs, LF-3-88 was identified as a potent nicotinic acetylcholine receptor (nAChR) partial agonist with subnanomolar to nanomolar affinities for β2-containing nAChRs (α2β2, α3β2, α4β2, and α4β2*) and superior selectivity away from α3β4 - (K i > 10(4) nmol/L) and α7-nAChRs (K i > 10(4) nmol/L) as well as 51 other central nervous system (CNS)-related neurotransmitter receptors and transporters. Functional activities at different nAChR subtypes were characterized utilizing (86)Rb(+) ion efflux assays, two-electrode voltage-clamp (TEVC) recording in oocytes, and whole-cell current recording measurements.

Spectrophotometric determination of molybdenum in steels with o-nitrophenylfluorone and cetyltrimethylammonium bromide.

A method has been developed for determining microamounts of molybdenum(VI) in aqueous solution by means of the Mo-o-nitrophenylfluorone-cetyltrimethylammonium bromide system, in which micellar solubilization is applied. A red complex is formed in 0.2-0.