Synthesis and cytotoxicity studies of novel -arylbenzo[]quinazolin-2-amines.

In this paper, we report a short and efficient synthesis of novel -arylbenzo[]quinazoline-2-amines. We have prepared a focused library of nineteen representative examples which have been submitted to cytotoxicity assays against a representative panel of eight cancer cell lines and several molecules gave attractive results in this area.

Sol-Gel TiO Thin Film on Au Nanoparticles for Heterogeneous Plasmonic Photocatalysis.

A new, simple method for preparing substrates for photocatalytic applications under visible light is presented. It is based on the preparation of a dense array of gold nanoparticles (AuNPs) by thermal dewetting of a thin gold film followed by spin-coating of a thin TiO film prepared by sol-gel chemistry. The photocatalytic properties of these nanocomposite films are studied by surface-enhanced Raman spectroscopy (SERS) following the N-demethylation reaction of methylene blue as a model reaction.

One-Pot Synthesis of -Fused Benzimidazo-β-carbolines through Sequential Propargylation/-Cycloisomerization Approach.

The first sequential acid-catalyzed propargylation/base-mediated -cycloisomerization between indolyl-benzimidazoles and propargylic alcohols is described. This protocol enables the one-pot construction of -fused benzimidazo-β-carbolines in good yields. The synthetic utility of this approach is demonstrated by the assembly of an -helicene and also by a gram-scale reaction.

First record of the family Diplommatinidae Gray, 1847 (Gastropoda: Architaenioglossa) from Ecuador with description of a new Adelopoma Doering, 1885.

Diplommatinidae Gray, 1847, a family of minute cyclophoroid gastropods, is recorded from Ecuador for the first time. Adelopoma gracile Gree, sp. nov.

Fluorinated Benzofuran and Dihydrobenzofuran as Anti-Inflammatory and Potential Anticancer Agents.

Benzofuran and 2,3-dihydrobenzofuran scaffolds are heterocycles of high value in medicinal chemistry and drug synthesis. Targeting inflammation in cancer associated with chronic inflammation is a promising therapy. In the present study, we investigated the anti-inflammatory effects of fluorinated benzofuran and dihydrobenzofuran derivatives in macrophages and in the air pouch model of inflammation, as well as their anticancer effects in the human colorectal adenocarcinoma cell line HCT116.

Double-Docking Technique for Femtosecond Laser-Assisted Deep Anterior Lamellar Keratoplasty: A Retrospective Consecutive Case Series Study of Advanced Keratoconus.

Purpose: The aim of this study was to report the clinical outcomes and prognosis of femtosecond laser (FSL)-assisted double-docking deep anterior lamellar keratoplasty (DD-DALK) for advanced keratoconus (AK).

Methods: Records of consecutive patients with keratoconus who underwent FSL-assisted DALK (DD-DALK) were reviewed.

Results: We analyzed 37 eyes from 37 patients who underwent DD-DALK.

Acylsilane Directed Rh-Catalyzed Arene C-H Alkylation with Maleimides and Visible-Light-Induced Siloxycarbene-Amide Cyclization: [3 + 2] Carbo-Annulation in Ru Catalysis.

We herein demonstrate the acylsilane-directed Rh-catalyzed arene C-H bond alkylation with maleimides. The resulting derivatives were utilized in visible-light-induced intramolecular siloxycarbene-amide cyclization for the synthesis of new tricyclic γ-lactams. In parallel, we also harnessed the same acylsilane and maleimide units through [3 + 2] carbo-annulation by using Ru-catalysis.

Domino alkyne insertion/aldol reaction/aromatization of 2-alkynyl indole-3-carbaldehyde with 1,3-diketones: entry to 2-indolyl phenols.

A novel one-pot base-promoted insertion of indolyl 2-alkynes into a C-C single bond of 1,3-diketones, followed by intramolecular aldol reaction and dehydrative aromatization is described. This reaction cascade leads to the construction of 2-indolyl phenols involving the formation of the C1-C2 and C3-C4 bonds of phenols resulting from the formal insertion process with a good substrate scope. Further, these bifunctional compounds were used in a novel arylative annulation in the presence of Grignard reagents to provide chromeno-indole frameworks.

Self-Assembly of Soot Nanoparticles on the Surface of Resistively Heated Carbon Microtubes in Near-Hexagonal Arrays of Micropyramids.

Almost regular hexagonal arrays of microscopic pyramids consisting of soot nanoparticles are formed on the surface of graphitized hollow filaments, which are resistively heated to ∼1800-2400 °C under an Ar atmosphere containing trace amounts of oxygen (∼300 ppm). At higher temperatures ( > 2300 °C, approximately) the soot particles are represented mainly by multishell carbon nano-onions. The height and width of the pyramids are strongly dependent on the temperature of the resistive heating, diminishing from 5 to 10 μm at ≈ 1800 °C to ∼1 μm at 2300-2400 °C.

Discovery of potent dual ligands for dopamine D4 and σ1 receptors.

During our work on exploration of molecules with some piperidine-triazole scaffolds, we realized that our compounds display chemical similarity with some σ, as well as dopaminergic receptor ligands. Here we show that this series of molecules has indeed strong affinity both for σ1 and dopamine D4 receptors. Moreover, they appear selective towards σ2, dopamine paralogues D1, D2, D3 and D5 receptors and hERG channel.

Near-Infrared Laser Direct Writing of Conductive Patterns on the Surface of Carbon Nanotube Polymer Nanocomposites.

Near-infrared (NIR) laser annealing is used to write conductive patterns on the surface of polypropylene/multi-walled carbon nanotube nanocomposite (PP/MWCNT) plates. Before irradiation, the surface of the nanocomposite is not conductive due to the partial alignment of the MWCNT, which occurs during injection molding. We observe a significant decrease in the surface sheet resistance using NIR laser irradiation, which we explain by a randomization of the orientation of MWCNTs in the PP matrix melt by NIR laser irradiation.

Synthesis and biological studies of new piperidino-1,2,3-triazole hybrids with 3-aryl isoxazole side chains.

A small library of new piperidine-triazole hybrids with 3-aryl isoxazole side chains has been designed and synthesized. Their cytotoxicity against a panel of seven cancer cell lines has been established. For the most promising compound, an IC value of 3.

Domino Reaction of 2,4-Diyn-1-ols with 1,3-Dicarbonyl Compounds: Direct Access to Aryl/Heteroaryl-Fused Benzofurans and Indoles.

A domino propargylation/furanylation (intramolecular --cyclization)/benzannulation reaction of 2,4-diyn-1-ols with 1,3-dicarbonyl compounds has been developed for the first time. This provides a novel and effective method for the preparation of aryl/heteroaryl-fused benzofurans from easily accessible starting materials in a single step. The methodology was extended to pyrrolyl-benzannulation to obtain aryl/heteroaryl-fused indoles.

Discovery of DB18, a potent inhibitor of CLK kinases with a high selectivity against DYRK1A kinase.

We describe in this paper the synthesis of a novel series of anilino-2-quinazoline derivatives. These compounds have been screened against a panel of eight mammalian kinases and in parallel they were tested for cytotoxicity on a representative panel of seven cancer cell lines. One of them (DB18) has been found to be a very potent inhibitor of human "CDC2-like kinases" CLK1, CLK2 and CLK4, with IC values in the 10-30 nM range.

In Vitro Degradation of Electrospun Poly(Lactic-Co-Glycolic Acid) (PLGA) for Oral Mucosa Regeneration.

Poly(lactic-co-glycolic acid) (PLGA) has been used in the field of tissue engineering as a scaffold due to its good biocompatibility, biodegradability and mechanical strength. With the aim to explore the degradability of PLGA electrospun nonwoven structures for oral mucosa tissue engineering applications, non-irradiated and gamma irradiated nonwovens were immersed in three different solutions, in which simulated body fluid (SBF) and artificial saliva are important for future oral mucosa tissue engineering. The nonwovens were immersed for 7, 15 and 30 days in SBF, culture media (DMEM) and artificial saliva at 37 °C.

-Difluorobisarylic derivatives: design, synthesis and anti-inflammatory effect.

Introduction: New fluorinated diaryl ethers and bisarylic ketones were designed and evaluated for their anti-inflammatory effects in primary macrophages.

Methods: The synthesis of the designed molecules started from easily accessible and versatile -difluoro propargylic derivatives. The desired aromatic systems were obtained using Diels-Alder/aromatization sequences and this was followed by Pd-catalyzed coupling reactions and, when required, final functionalization steps.

Metal-free propargylation/aza-annulation approach to substituted β-carbolines and evaluation of their photophysical properties.

An efficient acid-catalyzed propargylation/aza-annulation sequence was developed under metal-free reaction conditions, thus leading to a one-pot synthesis of a variety of substituted β-carbolines starting from propargylic alcohols and indole 2-carbonyls. This versatile strategy was further extended to the synthesis of 5-azaindoles and 5-azabenzothiazoles. Optical properties suggested that manipulation of electron donor and acceptor moieties on β-carbolines has an impact on their ground and excited state electronic behavior.

A thiosemicarbazone derivative induces triple negative breast cancer cell apoptosis: possible role of miRNA-125a-5p and miRNA-181a-5p.

Background: Breast cancer, the most commonly diagnosed malignancy in women, accounts for the highest cancer-related deaths worldwide. Triple negative breast cancer (TNBC), lacking the expression of estrogen, progesterone and HER2 receptors, has an aggressive clinical phenotype and is susceptible to chemotherapy but not to hormonal or targeted immunotherapy. In an attempt to identify potent and selective anti-TNBC agents, a set of thiosemicarbazone derivatives were screened for their cytotoxic activity against MDA-MB 231 breast cancer cell line.

Strategies towards the synthesis of anti-tuberculosis drugs.

Antituberculosis drugs have captured the attention of the scientific community due to the emergence of drug resistance. Hence, the development of new analogs and new drugs which can treat drug-resistant tuberculosis is required. In this report, we reviewed the strategies towards the synthesis of antituberculosis drugs.

Targeting PUMA/Bcl-xL interaction by new specific compounds to unleash apoptotic process in cancer cells.

We describe the first examples of small molecules able to disrupt the nanomolar interaction between the pro-apoptotic protein PUMA and its anti-apoptotic counterpart BcL-xL in malignant cells. Based on molecular modelling studies, we propose a rationale to this result, through a new "bottle-opener"-type strategy which could be of general use in the area of protein-protein interaction studies.

Synthesis and biological evaluation of longanlactone analogues as neurotrophic agents.

Longanlactone analogues were synthesized using a route featuring Friedel-Crafts acylation, Sonogashira coupling and 1,3-dipolar cycloaddition reactions. Structure-activity relationships were investigated for neurotrophic activity. Compound 6 was found to have the most potent neurotrophic activity among all the synthesized analogues in Neuro2a cells as evidenced by a battery of in vitro/cell based assays for assessment of neurogenic and potential neurotrophic activity including neurite outgrowth assay and real time PCR for popular markers of augmented neurotrophic activity.

Preparation of imidazo[1,2-]--heterocyclic derivatives with -difluorinated side chains.

Using an aerobic oxidative coupling, different new imidazo[1,2-]--heterocycles with -difluroroalkyl side chains have been prepared in fair yields by the reaction of -difluoroenones with aminopyridines, -pyrimidines and -pyridazines. Condensed heterocycles of this type play an important role as key core structures of various bioactive compounds. Further, starting with a chloroimidazopyridazine derivative, Pd-catalyzed coupling reactions as well as nucleophilic substitutions have been performed successfully in order to increase the molecular diversity.

Time-programmed release of fluoroscein isocyanate dextran from micro-pattern-designed polymer scrolls.

In this article we present a relevant strategy for a non-trivial time-programmed release of water-soluble macromolecules from biocompatible μ-containers. The system is based on self-scrolled chitosan acetate (CA) fibers, encapsulated in a poly(dimethylsiloxane) matrix. Mass transfer between a fiber and the external environment takes place via the only opened extremity of the fiber.