Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones.

A series of forty-six 5,6-annulated 2-arylthieno [2,3-d]pyrimidin-4(3H)-ones were prepared as potentially pleiotropic anticancer drugs with variance in the tubulin-binding trimethoxyphenyl motif at C-2 of a thieno [2,3-d]pyrimidine fragment, enlarged by additional rings of different size and substitution. By assessing their cytotoxicity against various cancer cells, their influence on the polymerization of neat tubulin and the dynamics of microtubule and F-actin cytoskeletons, and their vascular-disrupting and anti-angiogenic activities in vitro and in vivo, structure-activity relations were identified which suggest the 3-iodo-4,5-dimethoxyphenyl substituted thienopyrimidine 2e as a promising anticancer drug candidate for further research. 2020 Elsevier Ltd.

The in vivo mechanics of the magnetotactic backbone as revealed by correlative FLIM-FRET and STED microscopy.

Protein interaction and protein imaging strongly benefit from the advancements in time-resolved and superresolution fluorescence microscopic techniques. However, the techniques were typically applied separately and ex vivo because of technical challenges and the absence of suitable fluorescent protein pairs. Here, we show correlative in vivo fluorescence lifetime imaging microscopy Förster resonance energy transfer (FLIM-FRET) and stimulated emission depletion (STED) microscopy to unravel protein mechanics and structure in living cells.

Keeping the shoot above water - submergence triggers antithetical growth responses in stems and petioles of watercress (Nasturtium officinale).

The molecular mechanisms controlling underwater elongation are based extensively on studies on internode elongation in the monocot rice (Oryza sativa) and petiole elongation in Rumex rosette species. Here, we characterize underwater growth in the dicot Nasturtium officinale (watercress), a wild species of the Brassicaceae family, in which submergence enhances stem elongation and suppresses petiole growth. We used a genome-wide transcriptome analysis to identify the molecular mechanisms underlying the observed antithetical growth responses.

Synthesis, structures and cytotoxic effects in vitro of cis- and trans-[PtCl(NHC)] complexes and their Pt precursors.

Four new bis(N,N-dialkylbenzimidazol-2-ylidene)dichlorido platinum(ii) complexes 2 featuring N-alkyl substituents of increasing size (a: Me, b: Et, c: n-butyl, d: n-octyl) were synthesised and oxidised with PhICl to give the corresponding [PtCl(N,N-dialkylbenzimidazol-2-ylidene)] complexes 4 as potential anticancer prodrugs. The known bis(N,N-dibenzylimidazol-2-ylidene)dichlorido platinum(ii) complex 1 was likewise oxidised to [PtCl(N,N-dibenzylimidazol-2-ylidene)] 3. In contrast, oxidation of complexes 1 and 2 with HO or hypochlorites, or exchange of chlorido for hydroxo ligands in tetrachlorido complexes 4 failed to give isolable complexes of type [PtCl(OH)(NHC)].

Luminescent Gold(I) Complexes of 1-Pyridyl-3-anthracenylchalcone Inducing Apoptosis in Colon Carcinoma Cells and Antivascular Effects.

The luminescent chalcone gold(I) conjugates [Au(PPh)(AN3)]PF() and [Au(SIMes)(AN3)]PF () (AN3 = ()-3-(9-anthracenyl)-1-(4-pyridyl)propenone; SIMes = ,'-dimesitylimidazolidin-2-ylidene; Mes = 2,4,6-trimethylphenyl)) were prepared and characterized; complex was also characterized by X-ray crystallography. In MTT assays against a panel of three human colon, a melanoma and a breast cancer cell lines both complexes were antiproliferative with low micromolar IC values. It is noteworthy that HCT116 colon carcinoma cells lacking functional p53 (a vital tumor suppressor) were more susceptible to them than the wildtype parent cell line.

Abundance and distribution of large microplastics (1-5 mm) within beach sediments at the Po River Delta, northeast Italy.

Coastal areas are especially prone to plastic debris, being subjected to various land- and sea-based sources. Nevertheless, knowledge about microplastic distribution on beaches is limited, as studies focused either on high tide lines, specific items, or relied on visual identification. Beaches exhibit several accumulation zones and microplastic deposition depends on particle properties.

AtERF#111/ABR1 is a transcriptional activator involved in the wounding response.

AtERF#111/ABR1 belongs to the group X of the ERF/AP2 transcription factor family (GXERFs) and is shoot specifically induced under submergence and hypoxia. It was described to be an ABA-response repressor, but our data reveal a completely different function. Surprisingly, AtERF#111 expression is strongly responsive to wounding stress.

Pushing data quality for laboratory pair distribution function experiments.

Over the last decade, some studies with laboratory pair distribution function (PDF) data emerged. Yet, limited Q or instrumental resolution impeded in-depth structural refinements. With more advanced detector technologies, the question arose how to design novel PDF equipment for laboratories that will allow decent PDF refinements over r = 1-70 Å.

Chemical Modification and Foam Processing of Polylactide (PLA).

Polylactide (PLA) is known as one of the most promising biopolymers as it is derived from renewable feedstock and can be biodegraded. During the last two decades, it moved more and more into the focus of scientific research and industrial use. It is even considered as a suitable replacement for standard petroleum-based polymers, such as polystyrene (PS), which can be found in a wide range of applications-amongst others in foams for packaging and insulation applications-but cause strong environmental issues.

Multiple plant diversity components drive consumer communities across ecosystems.

Humans modify ecosystems and biodiversity worldwide, with negative consequences for ecosystem functioning. Promoting plant diversity is increasingly suggested as a mitigation strategy. However, our mechanistic understanding of how plant diversity affects the diversity of heterotrophic consumer communities remains limited.

One-trial learning in larval .

Animals of many species are capable of "small data" learning, that is, of learning without repetition. Here we introduce larval as a relatively simple study case for such one-trial learning. Using odor-food associative conditioning, we first show that a sugar that is both sweet and nutritious (fructose) and sugars that are only sweet (arabinose) or only nutritious (sorbitol) all support appetitive one-trial learning.

Effects of rain shortage on carbon allocation, pools and fluxes in a Mediterranean shrub ecosystem - a C labelling field study.

Hydrological cycle is expected to become the primary cause of ecosystem's degradation in near future under changing climate. Rain manipulation experiments under field conditions provide accurate picture on the responses of biotic processes to changed water availability for plants. A field experiment, mimicking expected changes in rain patterns, was established in a Mediterranean shrub community at Porto Conte, Italy, in 2001.

Microstructure and Mechanical Properties of Precipitate Strengthened High Entropy Alloy AlCoCrFeNiTi with Additions of Hafnium and Molybdenum.

High entropy or compositionally complex alloys provide opportunities for optimization towards new high-temperature materials. Improvements in the equiatomic alloy AlCoCrCuFeNi (at.%) led to the base alloy for this work with the chemical composition AlCoCrFeNiTi (at.

Silicon increases the phosphorus availability of Arctic soils.

Phosphorus availability in soils is an important parameter influencing primary production in terrestrial ecosystems. Phosphorus limitation exists in many soils since a high proportion of soil phosphorus is stored in unavailable forms for plants, such as bound to iron minerals or stabilized organic matter. This is in spite of soils having a high amount of total soil phosphorus.

Coastal accumulation of microplastic particles emitted from the Po River, Northern Italy: Comparing remote sensing and hydrodynamic modelling with in situ sample collections.

Microplastic research has mainly concentrated on open seas, while riverine plumes remain largely unexplored despite their hypothesized importance as a microplastic source to coastal waters. This work aimed to model coastal accumulation of microplastic particles (1-5 mm) emitted by the Po River over 1.5 years.

New naphthopyran analogues of LY290181 as potential tumor vascular-disrupting agents.

A series of 19 analogues of the antiproliferative naphthopyran LY290181 were prepared for structure-activity relationship studies. We found the best activities for test compounds bearing small substituents at the meta position of the phenyl ring. The mode of action of LY290181 and eight new analogues was studied in detail.

N,N-Dialkylbenzimidazol-2-ylidene platinum complexes - effects of alkyl residues and ancillary cis-ligands on anticancer activity.

Eleven complexes of [(1,3-dialkylbenzimidazol-2-ylidene)LCl]Pt, with L = DMSO (8), PhP (9), (PhP) (10), and alkyl = Me (a), Et (b), Bu (c), octyl (d), were synthesised and tested for cellular accumulation, cytotoxicity, interference with the tumour cell cycle, and interaction with DNA. The delocalised lipophilic cationic bisphosphane complexes 10 were on average found to be more cytotoxic in MTT assays against a panel of seven cancer cell lines than the neutral DMSO and monophosphane complexes 8 and 9. The uptake of complexes 10, at least into HCT116 colon carcinoma cells, was also significantly greater than that of analogues 8 and 9.

Black carbon yields highest nutrient and lowest arsenic release when using rice residuals in paddy soils.

Rice straw increasingly remains on the fields for nutrient supply to the next generation of crop plants. It can be applied either fresh or after burning to black carbon or ash. A central concern during rice cultivation is accumulation of carcinogenic arsenic and the question arises how much rice straw application contributes to nutrient versus arsenic supply in paddy fields.

Arabidopsis phytochrome A nuclear translocation is mediated by a far-red elongated hypocotyl 1-importin complex.

Phytochrome A (phyA) is a red and far-red (FR) sensing photoreceptor regulating plant growth and development. Its biologically active FR-absorbing form Pfr translocates into the nucleus and subsequently regulates gene expression. Two transport facilitators, FR elongated hypocotyl 1 (FHY1) and FHY1-like (FHL), are crucial for its cytoplasmic-nuclear translocation.

Entropy Determination of Single-Phase High Entropy Alloys with Different Crystal Structures over a Wide Temperature Range.

We determined the entropy of high entropy alloys by investigating single-crystalline nickel and five high entropy alloys: two fcc-alloys, two bcc-alloys and one hcp-alloy. Since the configurational entropy of these single-phase alloys differs from alloys using a base element, it is important to quantify the entropy. Using differential scanning calorimetry, c-measurements are carried out from -170 °C to the materials' solidus temperatures T.

Tensile Behavior and Evolution of the Phases in the AlCoCrFeNiTi Compositionally Complex/High Entropy Alloy.

Compositionally complex alloys, or high entropy alloys, are good candidates for applications at higher temperatures in gas turbines. After their introduction, the equiatomic AlCoCrCuFeNi (at.%) served as a starting material and a long optimization road finally led to the recently optimized AlCoCrFeNiTi (at.

A Supramolecular Crosslinker To Give Salt-Resistant Polyion Complex Micelles and Improved MRI Contrast Agents.

Three-component mixtures (diblock copolymer/metal ion/oligoligand) can assemble into micellar particles owing to a combination of supramolecular polymerization and electrostatic complex formation. Such particles cover a large range of compositions, but the electrostatic forces keeping them together make them rather susceptible to disintegration by added salt. Now it is shown how the salt stability can be tuned continuously by employing both a bis-ligand and a tris-ligand, and varying the ratio of these in the mixture.

Synthesis of the Entomopathogenic Fungus Metabolites Militarinone C and Fumosorinone A.

Militarinone C and fumosorinone A, 3-oligoenoyltetramic acids produced by insect pathogenic fungi, were synthesized for the first time. The pyrrolidine-2,4-dione ring was closed through a late-stage Dieckmann condensation of N-(β-ketoacyl) derivatives of tyrosine, obtained by its acylation with either thioesters or Meldrum's acid derivatives bearing the all- trans-polyene side chain. The latter was built up from ( S)-citronellol via an Evans methylation and Wittig or HWE olefinations.

Biomedical Applications of Recombinant Silk-Based Materials.

Silk is mostly known as a luxurious textile, which originates from silkworms first cultivated in China. A deeper look into the variety of silk reveals that it can be used for much more, in nature and by humanity. For medical purposes, natural silks were recognized early as a potential biomaterial for surgical threads or wound dressings; however, as biomedical engineering advances, the demand for high-performance, naturally derived biomaterials becomes more pressing and stringent.

Total Synthesis of the Diglycosidic Tetramic Acid Ancorinoside A.

Ancorinoside A, a metabolite of a sponge Ancorina sp., was prepared in 18 steps as the first derivative of this class of glycosylated 3-acyltetramic acids. It features a β-d-glucopyranosyl-(1→4)-β-d-galacturonic acid linked to a d-aspartic acid derived tetramic acid via a 3-docosanoyl spacer.