Latest ArticlesDrug resistance remains to be a serious problem with type I human immunodeficiency virus (HIV-1) non-nucleoside reverse transcriptase inhibitors (NNRTIs). A series of novel boronic acid-containing diarylpyrimidine (DAPY) derivatives were designed via bioisosterism and scaffold-hopping strategies, taking advantage of the ability of a boronic acid group to form multiple hydrogen bonds. The target compounds were synthesized and evaluated for their anti-HIV activities and cytotoxicity in MT-4 cells. Compound 10j yielded the most potent activity and turned out to be a single-digit nanomolar inhibitor towards the HIV-1 IIIB [wild-type (WT) strain], L100I and K103N strains, with 50% effective concentration (EC50) values of 7.19–9.85 nmol/L. Moreover, 10j inhibited the double-mutant strain RES056 with an EC50 value of 77.9 nmol/L, which was 3.3-more potent than that of EFV (EC50 = 260 nmol/L) and comparable to that of ETR (EC50 = 32.2 nmol/L). 10j acted like classical NNRTIs with high affinity for WT HIV-1 reverse transcriptase (RT) with 50% inhibition concentration (IC50) value of 0.1837 μmol/L. Furthermore, molecular dynamics simulation indicated that 10j was proposed as a promising molecule for fighting against HIV-1 infection through inhibiting RT activity. Overall, the results demonstrated that 10j could serve as a lead molecule for further modification to address virus-drug resistance.
Three matrine-derived alkaloids, alopecuroidine A (1), alopecuroidine B (2a) and alopecuroidine C (2b) were isolated from the seeds of Sophora alopecuroides. Their structures were elucidated by extensive spectroscopic analyses and X-ray diffraction. Three compounds possess an unprecedented rearranged fused 7/6/5/6 tetracyclic skeleton with a diazacycloheptane structure. Their plausible biosynthetic pathway was also proposed. The anti-proliferative activities of compounds 1 and 2a were examined by the MTT assay. Compound 1 inhibited the viability of human lung cancer A549 cells, having a half maximal inhibitory concentration (IC50) of 7.58 ± 2.47 µmol/L at 72 h. The flow cytometric analysis suggested that 1 inhibited A549 cell growth by inducing apoptosis and cell-cycle arrest. Additionally, 1 induced the loss of mitochondrial membrane potential, elevated intracellular reactive oxygen species, increased the Bax/Bcl-2 ratio, stimulated cleaved-caspase-3 and P53 protein levels, and suppressed the pro-caspase-3 level. Thus, 1 appeared to induce A549 cells apoptosis through a mitochondria-mediated apoptotic pathway.
Cu-catalyzed endo-selective asymmetric 1,3-dipolar cycloaddition of azomethine ylides with ethenesulfonyl fluorides (ESFs) was successfully developed, this protocol provided an efficient and facile method to a wide range of chiral pyrrolidine-3-sulfonyl fluorides with good to excellent results (up to 87% yield, > 20:1 dr, 94% ee). Some other chiral sulfonyl derivatives, such as sulfonamide and sulfonate, were easily accessible through simple transformations with high yields, which demonstrated that the cycloaddition products could be synthetically useful in the sulfur(Ⅵ) fluoride exchange (SuFEx) chemistry.
Carbon dots (CDs), as a new member of carbon nanostructures, have been widely applied in extensive fields due to their exceptional physicochemical properties. While, the emissions of most reported CDs are located in the blue to green range under the excitation of ultraviolet or blue light, which severely limits their practical applications, especially in photovoltaic and biological fields. Studies that focused on synthesizing CDs with long-wavelength (red to near-infrared) emission/excitation features (simply named L-w CDs) and exploring their potential applications have been frequently reported in recent years. In this review, we analyzed the key influence factors for the synthesis of CDs with long wavelength and multicolor (containing long wavelength) emissive properties, discussed possible fluorescence mechanism, and summarized their applications in sensing and cancer theranostics. Finally, the existing challenges and potential opportunities of L-w CDs are presented.
Zn-ion batteries (ZIBs) have gained great attention as promising next-generation power sources, because of their low cost, enviable safety and high theoretical capacity. Recently, massive researches have been devoted to vanadium-based materials as cathodes in ZIBs, owing to their multiple valence states, competitive gravimetric energy density, but the capacity degradation, sluggish kinetics, low operating voltage hinder further optimization of their performance in ZIBs. This review summarizes recent progress to increase the interlayer spacing, structural stability, and the diffusion ability of the guest Zn ions, including the insertion of different ions, introduction of defects, design of diverse morphologies, the combination of other materials. We also focus on approaches to promoting the valuable performance of vanadium-based cathodes, along with the related ongoing scientific challenges and limitations. Finally, the future perspectives and research directions of vanadium-based aqueous ZIBs are provided.
Thrombotic disease is a major problem that endangers human health. At present, MRI and CT are commonly used clinically to diagnose thrombosis, and thrombolytic drugs are used for treatment), but the diagnosis time is lagging, the utilization of drugs is low, and the resulting systemic toxicity problems such as side effects lead to poor treatment effects. Nanotechnology combining photoacoustic dynamics and chemical dynamics has shown great application value in tumor targeting, diagnosis, detection and treatment. It has also become a new direction in the diagnosis and treatment of thrombotic diseases, and has created new applications in the field of nanomaterials. This review summarizes the new progress of this combination in the diagnosis and treatment of thrombotic diseases according to the differences in the construction of the nanotherapy system, at the same time, we put forward some new problems and prospects for the integration of thrombosis diagnosis and treatment.
Supercapacitors (SCs) with high power density and long cycling span life are demanding energy storage devices that will be an attractive power solution to modern electronic and electrical applications. Numerous theoretical and experimental works have been devoted to exploring various possibilities to increase the functionality and the specific capacitance of electrodes for SCs. Non-carbon two-dimensional (2D) materials have been considered as encouraging electrode candidates for their chemical and physical advantages such as tunable surface chemistry, high electronic conductivity, large mechanical strength, more active sites, and dual non-faradaic and faradaic electrochemical performances. Besides, these 2D materials also play particular roles in constructing highway channels for fast ion diffusion. This concise review summarizes cutting-edge progress of some representative 2D non-carbon materials for the aqueous electrolyte-based SCs, including transition metal oxides (TMOs), transition metal hydroxides (TMHs), transition metal chalcogenides (TMCs), MXenes, metal-organic frameworks (MOFs) and some emerging materials. Different synthetic methods, effective structural designs and corresponding electrochemical performances are reviewed in detail. And we finally present a detailed discussion of the current intractable challenges and technical bottlenecks, and highlight future directions and opportunities for the development of next-generation high-performance energy storage devices.
Recent years have witnessed the wide contributions made by transition metal dichalcogenides (TMDCs) to various fields, including the biomedical field. Here, to identify and further promote the development of biomedical TMDCs, we provide a bibliometric analysis of literature regarding TMDCs for biomedical applications. Firstly, general bibliometric distributions of the dataset by year, country, institute, Web of Science category and referenced source are recognized. Following, we carefully explore the research hotspots of the TMDC-related biomedical field, among which biosensing, bioelectronics, cancer theranostics, antibacterial and tissue engineering are identified. The functions of TMDCs in each biomedical scenario, the related properties and research challenges are highlighted. Finally, future prospects are proposed to shed light on the design of novel TMDC-related biomaterials, potential new biomedical applications, as well as their clinical translation.
The scandocene alkyl complex (C5Me5)2ScCH2SiMe3 was found to be an efficient catalyst for the dehydrocoupling of the non-cyclic boranes, dicyclohexylborane and thexylborane, with amines under mild conditions. The reactions afforded the corresponding aminoboranes in high yields with good functional group tolerance. The stoichiometric reaction of scandium alkyl with amine led to the isolation of a scandium amide complex, which was shown to be an active species during the catalysis. Although a borane-coordinated scandium hydride was also obtained from the stoichiometric experiment, it was not involved in the catalytic cycle. In addition, kinetic studies provided insight into this intermolecular dehydrogenation reaction.
Three carbazole derivatives, AcPTC, PxPTC and PtPTC, consisting of two 9,9-dimethyl-9,10-dihydroacridine, phenoxazine or phenothiazine donor groups and one diphenyltriazine acceptor group fixed at 1,8,9-positions of a single carbazole ring via phenylene, are designed and synthesized. X-ray diffraction analysis of AcPTC reveals that there exist multiple π-π interactions between the donor and acceptor groups to form a sandwich-like structural unit with edge-to-face interaction model. The compounds thus show obvious thermally activated delayed fluorescence with through-space charge transfer character and possess considerable photoluminescence quantum yields of up to 73% in doped films with sky-blue to yellow emissions. The solution-processed electroluminescent devices achieve the highest maximum external quantum efficiencies of 10.0%, 11% and 5.6% for AcPTC, PxPTC and PtPTC, respectively, with small efficiency roll-offs.
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