Vascular endothelial growth factor receptor‐2 (VEGFR‐2) plays an important role in both vasculogenesis and angiogenesis. Inhibition of VEGFR‐2 has been demonstrated as a key method against tumor‐associated angiogenesis. Thiazolopyrimidine is an important analog of the purine ring, and we choose the thiazolopyrimidine scaffold as the mother nucleus. Two series of thiazolo[5,4‐d]pyrimidine derivatives were synthesized and evaluated for their antiproliferative activity. In HUVEC inhibition assay, compounds 3l (=1‐(5‐{[2‐(4‐chlorophenyl)‐5‐methyl[1,3]thiazolo[5,4‐d]pyrimidin‐7‐yl]amino}pyridin‐2‐yl)‐3‐(3,4‐dimethylphenyl)urea) and 3m (=1‐(5‐{[2‐(4‐chlorophenyl)‐5‐methyl[1,3]thiazolo[5,4‐d]pyrimidin‐7‐yl]amino}pyridin‐2‐yl)‐3‐(4‐methoxyphenyl)urea) exhibited the most potent inhibitory effect (IC50=1.65 and 3.52 μm , respectively). Compound 3l also showed the best potency against VEGFR‐2 at 50 μm (98.5 %). These results suggest that further investigation of compound 3l might provide potential angiogenesis inhibitors. 相似文献
Carbonaceous materials are widely employed to host Li for stable and safe Li metal batteries while relatively little effort is devoted to tailoring the surface properties of carbon to facilitate uniform Li plating. Herein, the correlation between Li plating behavior and the surface characteristics of electrospun porous carbon nanofibers (PCNFs) is systemically elucidated through experiments and theoretical calculations. It is revealed that the neat carbon surface suffers from severe lattice mismatch with Li metal, hindering uniform Li plating. In contrast, open pores created on the PCNF surface serve as active sites for controlled initial nucleation of Li. The introduction of oxygenated functional groups further facilitates the nucleation of Li on PCNFs through the largely reduced nucleation energy barrier. The Li film uniformly deposited on PCNFs enables efficient use of the whole carbon surface, giving rise to enhanced cyclic stability of the electrode. When used as an anode in lithium–sulfur batteries, the modified electrode delivers an excellent energy density of 385 Wh kg?1 after 100 cycles. The fundamental correlation established in this study is universal to all types of carbonaceous materials and sheds new light on the rational design of high‐performance Li metal anodes by controlling the initial Li nucleation. 相似文献
Marker‐based prediction holds great promise for improving current plant and animal breeding efficiencies. However, the predictabilities of complex traits are always severely affected by negative factors, including distant relatedness, environmental discrepancies, unknown population structures, and indeterminate numbers of predictive variables. In this study, we utilised two independent F1 hybrid populations in the years 2012 and 2015 to predict rice thousand grain weight (TGW) using parental untargeted metabolite profiles with a partial least squares regression method. A stable predictive model for TGW was built based on hybrids from the population in 2012 (r = 0.75) but failed to properly predict TGW for hybrids from the population in 2015 (r = 0.27). After integrating hybrids from both populations into the training set, the TGW of hybrids could be predicted but was largely dependent on population structures. Then, core hybrids from each population were determined by principal component analysis and the TGW of hybrids in both environments were successfully predicted (r > 0.60). Moreover, adjusting the population structures and numbers of predictive analytes increased TGW predictability for hybrids in 2015 (r = 0.72). Our study demonstrates that the TGW of F1 hybrids across environments can be accurately predicted based on parental untargeted metabolite profiles with a core hybridisation strategy in rice. Metabolic biomarkers identified from early developmental stage tissues, which are grown under experimental conditions, may represent a workable approach towards the robust prediction of major agronomic traits for climate‐adaptive varieties. 相似文献
The reduction of nuclear fast red (NFR) stain by sodium tetrahydroboron was catalyzed in the presence of silver ions (Ag+). The fluorescence properties of reduced NFR differed from that of NFR. The product showed fluorescence emission at 480 nm with excitation at 369 nm. Furthermore, the fluorescence intensity of the mixture increased strongly in the presence of Ag+ and Britton–Robinson buffer at pH 4.78. There was a good linear relationship between increased fluorescence intensity (ΔI) and Ag+ concentration in the range 5.0 × 10?9 to 5.0 × 10?8 M. The correlation coefficient was 0.998, and the detection limit (3σ/k) was 1.5 × 10?9 M. The colour of the reaction system changed with variation in Ag+ concentration over a wide range. Based on the colour change, a visual semiquantitative detection method for recognition and sensing of Ag+ was developed for the range 1.0 × 10?8 to 5.0 × 10?4 M, with an indicator that was visible to the naked eye. Therefore, a sensitive, simple method for determination of Ag+ was developed. Optimum conditions for Ag+ detection, the effect of other ions and the analytical application of Ag+ detection of synthesized sample were investigated. 相似文献
Due to their large-scale manufacture and widespread application, there have been a number of studies related to toxicological assessment of nanomaterials (NMs) over the past decade. Although there has been extensive research on the cytotoxicity of NMs, concerns have been raised about their possible genotoxicity. The genome is constantly exposed to genotoxic insults that can lead to DNA damage, which in turn can have consequences for health, such as the induction of carcinogenesis. This comprehensive review focuses on the direct and indirect interactions of NMs with DNA. Factors influencing the genotoxicity of NMs, such as their physicochemical characteristics, are also discussed. The mechanisms involved in the direct and indirect interactions of NMs with DNA are also reviewed. Many studies have shown that ENMs have genotoxic effects, such as chromosomal fragmentation, DNA strand breaks, point mutations, oxidative DNA adducts, apoptosis, hypoxic responses, mitochondrial dysfunction, and epigenetic modifications. As the data reported to date are inconsistent, it is difficult to draw definitive conclusions regarding the features of NMs that promote genotoxicity. Therefore, challenges and future research perspectives are discussed. This review provides insights into the genotoxic effects of NMs and their consequences for human health.