Photoredox/nickel dual-catalyzed regioselective alkylation of propargylic carbonates for trisubstituted allenes.

Herein, a highly regioselective alkylation of propargylic carbonates for trisubstituted allenes with alkyl 1,4-dihydropyridine derivatives (1,4-DHPs) is developed a photoredox/nickel dual-catalyzed process, which represents the first direct approach to access alkylated allene products without alkyl organometallic reagents. This method features a broad substrate scope and mild conditions. A hypothetical mechanism with an alkyl radical and an allenyl Ni(III) species is proposed.

Organic/Inorganic Hybrid Boosting Energy Harvesting Based on the Photothermoelectric Effect.

Attracted by the capability of light to heat and electricity conversion, the photothermoelectric (PTE) effect has drawn great attention in the field of energy conversion and self-powered electronics. However, it still requires effective strategies to convert electricity from light based on the corresponding photothermoelectric generator. Herein, considering the broad photoresponse and large Seebeck effect of tellurium nanowires (Te NWs) as well as the high electrical conductivity of poly(3,4-ethylenedioxythiophene):poly(styrenesulfonate) (PEDOT:PSS), PEDOT:PSS/Te NW hybrid thin films were fabricated to enhance the conversion efficiency by the photothermoelectric effect with respect to single thermoelectric performance.

Identification of ruthenium (II) complexes with furan-substituted ligands as possible antibacterial agents against Staphylococcus aureus.

The growing burden of antibiotic resistance worldwide calls for developing new classes of antimicrobial strategy. Recently years, the use of adjuvants that rescue antibiotics identified as a promising strategy for overcoming bacterial resistance. In this study, three ruthenium complexes functionalized with furan-substituted ligands([Ru(phen) (CAPIP)](ClO ) (Ru(Ⅱ)-1), [Ru(dmp) (CAPIP)](ClO ) (Ru(Ⅱ)-2) and [Ru(dmb) (CAPIP)](ClO ) (Ru(Ⅱ)-3) (dmb=4,4'-dimethyl-2,2'-bipyridine, phen=1,10-phenanthroline, dmp=2,9-dimethyl-1,10-phenanthroline, CAPIP=(E)-2- (2-(furan-2-yl)vinyl)-1H-imidazo[4,5-f][1,10]phenanthroline)) were designed and synthesized.

Purification and Characterization of a Novel Fibrinolytic Enzyme from Cipangopaludina Cahayensis.

Background: Cipangopaludina cahayensis contains active fibrinolytic proteins and has been considered a potential anti-cancer agent. However, its anti-cancer characteristics and functions have yet to be elucidated.

Objectives: To study the fibrinolytic activity and anticancer activity of crude protein extracts from Cipangopaludina cahayensis.

Design, synthesis, docking, molecular dynamics and bioevaluation studies on novel N-methylpicolinamide and thienopyrimidine derivatives with inhibiting NF-κB and TAK1 activities: Cheminformatics tools RDKit applied in drug design.

Using cheminformatics tools RDKit and literature investigation, four series of 24 thienopyrimidine/N-methylpicolinamide derivatives substituted with pyrimidine were designed, synthesized and evaluated for activities against three cancer cell lines (MDA-MB-231, HCT116 and A549), TAK1 kinase and NF-κB signaling pathway. Almost all compounds showed selectivity toward the A549 cell lines and the most promising compound 38 could inhibit TAK1 kinase and NF-κB signaling pathway with the IC values of 0.58 and 0.

The GRAS gene family in watermelons: identification, characterization and expression analysis of different tissues and root-knot nematode infestations.

The family of GRAS plant-specific transcription factor plays diverse roles in numerous biological processes. Despite the identification and characterization of GRAS genes family in dozens of plant species, until now, GRAS members in watermelon () have not been investigated comprehensively. In this study, using bioinformatic analysis, we identified 37 GRAS genes in the watermelon genome (ClGRAS).

Regulating monomer assembly to enhance PEDOT capacitance performance via different oxidants.

The development of poly(3,4-ethylenedioxythiophene) (PEDOT) with high specific capacitance is the key to pursuing high-performance supercapacitors, and the electrochemical properties of PEDOT are closely related to the oxidation degree and conjugated chain length of its molecular chain. In this work, the influences of various oxidants (FeCl, Fe(Tos) and MoCl) on the molecular chain structure and capacitive properties of PEDOT via vapor phase polymerization were systematically investigated. Fe(Tos) can significantly improve the degree of oxidation and the length of the conjugated chain of PEDOT compared to FeCl and MoCl, enhancing the conductivity and providing more active sites for Faraday reaction.

Evaluation of candidate reference genes for gene expression analysis in the brassica leaf beetle, Phaedon brassicae (Coleoptera: Chrysomelidae).

The brassica leaf beetle Phaedon brassicae is a notorious defoliator of cruciferous vegetables. However, few molecular studies of this pest have been conducted due to limited sequence data. Recently, RNA sequencing has offered a powerful platform to generate numerous transcriptomic data, which require RT-qPCR to validate target gene expression.

Design, Synthesis, and Antitumor Activity of Olmutinib Derivatives Containing Acrylamide Moiety.

Two series of olmutinib derivatives containing an acrylamide moiety were designed and synthesized, and their IC values against cancer cell lines (A549, H1975, NCI-H460, LO2, and MCF-7) were evaluated. Most of the compounds exhibited moderate cytotoxic activity against the five cancer cell lines. The most promising compound, , showed not only excellent activity against EGFR kinase but also positive biological activity against PI3K kinase.

A unique red-emitting molecular rotor for high-fidelity visualizing and long-term tracking mitochondria.

Visualizing and tracking mitochondrial changes is the key to understand the processes of diseases related to mitochondria, which is meaningful to physiology, pathology, and pharmacology. So, a great deal of mitochondrial probes was designed and synthesized according to the principle that probes with a positive charge can target mitochondria through mitochondrial membrane potential (MMP). However, these traditional mitochondrial probes are not able to visualize and track mitochondrial changes, because their targeting abilities depend on high MMP.

Synthesis of ruthenium complexes functionalized with benzothiophene and their antibacterial activity against Staphylococcus aureus.

New effective antimicrobial agents with novel modes of action are urgently needed due to the continued emergence of drug-resistant bacteria. Here, three ruthenium complexes functionalized with benzothiophene: [Ru(phen)(BTPIP)](ClO) (Ru(II)-1), [Ru(dmp)(BTPIP)](ClO) (Ru(II)-2) and [Ru(dmb)(BTPIP)](ClO) (Ru(II)-3) (dmb = 4,4'-dimethyl-2,2'-bipyridine, phen = 1,10-phenanthroline, dmp = 2,9-dimethyl-1,10-phenanthroline) have been synthesized and their antimicrobial activities in vitro were assessed. Minimum inhibitory concentration (MIC) assays indicated that the three Ru(II)-1, Ru(II)-2 and Ru(II)-3 complexes all showed antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa.

Design, synthesis and evaluation of anti-proliferative activity of 2-aryl-4-aminoquinazoline derivatives as EGFR inhibitors.

A class of 2-aryl-4-aminoquinazoline derivatives (7a-7j, 8a-8h, 9a-9h and 10a-10k) were designed, synthesized and evaluated as EGFR inhibitors. The anti-proliferative activity of compounds in vitro showed that compound 9e was considered to be a promising derivative. Compared with the lead compound Angew2017-7634-1, 9e exhibited excellent inhibitory activity against A549, NCI-H460 and H1975 cell lines, with IC values of 14.

Characterization and Quantification of Luteolin-Metal Complexes in Aqueous Extract of Lonicerae Japonicae Flos and Huangshan Wild Chrysanthemum.

Luteolin is a flavonoid compound widely found in vegetables, fruits, and medicinal plants. In this study, the reaction conditions for luteolin and five metal ions (Ca, Mg, Zn, Fe, and Cu) to form complexes in hot water were optimized, which was at a molar ratio of 1 : 1 for luteolin and metal ions at 90°C in a volume of 20 mL for 2 h, and the ability of luteolin to form complexes with Cu was the strongest. The DPPH scavenging test showed that luteolin exerted a dose-dependent effect on the clearance of free radicals; luteolin-Cu complexes and luteolin-Fe complexes accentuated the clearance of free radicals.

Visible light-driven novel BiTiO/CaTiO composite photocatalyst with enhanced photocatalytic activity towards NO removal.

Photocatalysis is regarded as a promising technology for removal of nitrogen oxide (NO), however, the low photocatalytic efficiencies under visible light irradiation and the deactivation of the photocatalyst are as yet the significant issues that should be addressed. In this work, visible-light-driven BiTiO/CaTiO heterojunction composites were synthesized by a facile in-situ hydrothermal method. The BiTiO/CaTiO composites displayed superior visible light photocatalytic activity than pure CaTiO and pure BiTiO in the removal of NO at the 600 ppb level in air.

Novel Functional Recombinant Human Follicle-Stimulating Hormone Acquired from Goat Milk.

An animal mammary bioreactor is regarded as an excellent biological system which is applied to produce large-scale recombinant proteins in milk. However, there are no effective methods to produce a large amount of some pharmaceutical proteins, such as human follicle-stimulating hormone (FSH), by large animal mammary gland bioreactors due to the fact that accumulation of excessive bioactive FSH might cause serious diseases in animals. Here, we report a novel strategy of preparing recombinant human FSH (rhFSH) from goat mammary glands, which could avoid the accumulation of bioactive FSH in goats.

Retraction: Functional disruption of staphylococcal accessory regulator A from by silver ions.

[This retracts the article DOI: 10.1039/D0RA06357F.].

Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidine derivatives containing 1,8-naphthyridine-4-one fragment.

In this study, a series of pyrrolo [2,3-d]pyrimidine derivatives containing 1,8-naphthyridine-4-one fragment were synthesized and their biological activity were tested. Most of the target compounds displayed moderate to excellent activity against one or more cancer cell lines and low activity against human normal cell LO2 in vitro. The most promising compound 51, of which the IC values were 0.

A technological innovation and economic progress enhancement: an assessment of sustainable economic and environmental management.

This study examines the role of technological innovation and economic progress on environmental pollution by using STRIPAT and EKC theoretical frameworks in 25 developing Asian countries from the period 1998 to 2019. For technological advancement, the energy intensity has been used to gauge how much of the quantity of energy is employed to produce the additional unit of gross domestic product at domestic level. Therefore, the volume of the energy used in the production process is highly important as it is documented through the energy intensity.

Flexible fiber-shaped hydrogen gas sensor via coupling palladium with conductive polymer gel fiber.

Rational design of fiber-shaped gas sensors with both excellent mechanical properties and sensing performance is of great significance for boosting future portable and wearable sensing electronics, however, it is still a challenge. Herein, we develop a novel fiber-shaped hydrogen (H) sensor by directly electrochemically growing palladium (Pd) sensing layer on conductive poly(3,4-ethylenedioxythiophene):poly(styrene sulfonate) (PEDOT:PSS) fiber electrode. This approach produces free-standing functional fiber (PEDOT:PSS@Pd) with promising mechanical features of flexibility, light weight, knittability and high mechanical strength, and good H sensing performance at room temperature.

Etiology of Hypospadias: A Comparative Review of Genetic Factors and Developmental Processes Between Human and Animal Models.

Hypospadias is a congenital anomaly of the penis with an occurrence of approximately 1 in 200 boys, but the etiology of the majority of hypospadias has remained unknown. Numerous genes have been reported as having variants in hypospadias patients, and many studies on genetic deletion of key genes in mouse genital development have also been published. Until now, no comparative analysis in the genes related literature has been reported.

Design, synthesis and biological evaluation of novel 4-(pyrrolo[2,3-d]pyrimidine-4-yloxy)benzamide derivatives as potential antitumor agents.

Cancer is a major cause of death worldwide. Small molecule inhibitors have become a major therapeutic treatment for cancer. In this study, a series of novel 4-(pyrrolo[2,3-d]pyrimidine-4-yloxy)benzamide derivatives were designed, synthesized and evaluated for their antitumor activity against the A549, Hela and MCF-7 cell lines.

Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors for the treatment of non-small cell lung cancer: a patent review (2014-present).

: EGFR is the receptor for epidermal growth factor (EGF) and belongs to the protein tyrosine kinase (PTK) receptor. It is closely related to the inhibition of tumor cell proliferation, invasion, and apoptosis. Overexpression or mutation activation of EGFR is involved in the development of many human malignancies, especially non-small cell lung cancer (NSCLC).

The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation.

Epidermal growth factor receptor (EGFR) is a receptor for epithelial growth factor (EGF) cell proliferation and signaling, which is related to the inhibition of tumor cell proliferation, angiogenesis, tumor invasion, metastasis, and apoptosis. Thus, it has become an important target for the treatment of non-small cell lung cancer (NSCLC). The first to the third-generation EGFR inhibitors have demonstrated powerful efficacy and brought a prospect to patients.

Identification and Expression Analysis of Sugar Transporter Gene Family in .

Sugar transporter (SUT) genes are associated with multiple physiological and biochemical processes in filamentous fungi, such as the response to various stresses. However, limited systematic analysis and functional information of SUT gene family have been available on (). To investigate the potential roles of SUTs in , we performed an integrative analysis of the SUT gene family in this study.