Synthesis and Anti-Breast Cancer Evaluation of Novel N-(Guanidinyl)benzenesulfonamides

Scientific and Technologial Innovation Programs of the Nanjing military region, China [10MA077]A series of 4-(substituted)-N-(guanidinyl)benzenesulfonamides bearing biologically active pyrazole, pyrimidine and pyridine moieties were prepared and evaluated for their anticancer activity against human tumor breast cell line (MCF7). These sulfonamides showed promising activity with IC50 values ranging from 49.5 to 70.2 mu M. The structure-activity relationship of the synthesized compounds was studied. Interestingly, it was found that the most potent compounds in this study were the corresponding 2-cyanoacrylate 3, 3-oxobutanoate 4, pyrazole 6, pyridine 9 and pyrazole 13. Compounds 7 and 8 are nearly as active as Doxorubicin as reference drug with (IC50 values = 70.2, 68.1 mu M), while compounds 5, 10 and 11 exhibited a moderate activity

A Comprehensive Review of One-Dimensional Metal-Oxide Nanostructure Photodetectors

One-dimensional (1D) metal-oxide nanostructures are ideal systems for exploring a large number of novel phenomena at the nanoscale and investigating size and dimensionality dependence of nanostructure properties for potential applications. The construction and integration of photodetectors or optical switches based on such nanostructures with tailored geometries have rapidly advanced in recent years. Active 1D nanostructure photodetector elements can be configured either as resistors whose conductions are altered by a charge-transfer process or as field-effect transistors (FET) whose properties can be controlled by applying appropriate potentials onto the gates. Functionalizing the structure surfaces offers another avenue for expanding the sensor capabilities. This article provides a comprehensive review on the state-of-the-art research activities in the photodetector field. It mainly focuses on the metal oxide 1D nanostructures such as ZnO, SnO2, Cu2O, Ga2O3, Fe2O3, In2O3, CdO, CeO2, and their photoresponses. The review begins with a survey of quasi 1D metal-oxide semiconductor nanostructures and the photodetector principle, then shows the recent progresses on several kinds of important metal-oxide nanostructures and their photoresponses and briefly presents some additional prospective metal-oxide 1D nanomaterials. Finally, the review is concluded with some perspectives and outlook on the future developments in this area

Silencing of Ether à Go-Go 1 by shRNA Inhibits Osteosarcoma Growth and Cell Cycle Progression

Recently, a member of the voltage-dependent potassium channel (Kv) family, the Ether à go-go 1 (Eag1) channel was found to be necessary for cell proliferation, cycle progression and tumorigenesis. However, the therapeutic potential of the Eag1 channel in osteosarcoma remains elusive. In the present study, a recombinant adenovirus harboring shRNA against Eag1 was constructed to silence Eag1 expression in human osteosarcoma MG-63 cells. We observed that Eag1-shRNA inhibited the proliferation and colony formation of MG-63 cells due to the induction of G1 phase arrest. Moreover, in vivo experiments showed that Eag1-shRNA inhibited osteosarcoma growth in a xenograft nude mice model. In addition, selective inhibition of Eag1 significantly decreased the expression levels of cyclin D1 and E. Taken together, our data suggest that the Eag1 channel plays a crucial role in regulating the proliferation and cell cycle of osteosarcoma cells, and represents a new and effective therapeutic target for osteosarcoma

Influence of different energetic plasticizers on the performance of NC-RDX nitramine gun propellants

Energetic plasticizers are an essential component of propellants and have a significant impact on their performance, such as energy, combustion, and mechanics. Therefore, there is significant practical value in understanding how plasticizers affect the performance of propellants. In this work, the glass transition temperatures of several energetic plasticizers were compared. By adding energetic plasticizers with good compatibility with the propellant and a low glass transition temperature to the propellant, nitramine gun propellants containing different energetic plasticizers were prepared through a semi-solvent method. The compatibility, thermal behavior, phase structure, composition, mechanical properties, energy, and combustion performance of the nitramine gun propellants were characterized. The influence of plasticizers on the phase structure of the propellant and its mechanism on the combustion performance of the propellant were discussed. Energetic plasticizers GAPE, DNPH, and BuNENA have good compatibility and chemical stability with NC-RDX and display good plasticization. GAPE–NC–RDX, DNPH–NC–RDX, and BuNENA–NC–RDX propellants exhibit stable combustion performance at −40 °C, 20 °C, and 50 °C. Compared with the nitramine gun propellant plasticized with NG, the impact strength of the propellant plasticized with DNPH and BuNENA increased by 108.1 % and 17.2 % at −40 °C, respectively. This work offers a solution to improve the phase structure, mechanical properties, and combustion stability of heterogeneous gun propellants and provides a way to suppress the excessive burning rate and flame temperature of propellants

Mechanism of the anisotropic nitroguanidine crystal arrangement on triple-base propellant failure by impact and strategy of structural enhancement

Nitroguanidine (NQ) in solvent-based triple-base propellants (STP) has a propensity to peel off and detach from the matrix, leading to significant defects, such as interface debonding within the propellant’s microstructure. This ultimately results in reduced and unstable mechanical properties. To address this critical issue, an efficient and eco-friendly manufacturing process was employed to successfully produce solventless triple-base propellants (SLTPs) as a comparison to conventional STPs. SLTP samples exhibit a mutually supportive three-dimensional spatial structure, with NQ crystals within the propellant matrix more securely bonded to the interface. They also demonstrate higher relative density (1.68 g·cm−3), more stable molding dimensions (no contraction), and enhanced tensile strength (41.92 MPa). Quasi-static structural failure tests reveal that the standard deviation of compressive strength for SLTP samples in three axes is smaller, registering at 1.10. The dynamic structural damage performance analysis indicates that the failure of energetic composite materials is attributable to separation fracture damage after the appearance of cracks on the tensile surface at −40 and 25 °C. Furthermore, the structural failure of these materials occurs due to significant collapse failure after the compression surface bends inward at 50 °C. Consequently, the present study offers a reliable theoretical foundation and procedural strategy for enhancing the structural strength of triple-base propellants