Epigenetic alterations found in all human cancers are promising targets for anticancer therapy. In this sense, histone deacetylase inhibitors (HDACIs) are interesting anticancer agents that play an important role in the epigenetic regulation of cancer cells. Here, we report 15 novel hydroxamic acid-based histone deacetylase inhibitors with quinazolinone core structures. Five compounds exhibited antiproliferative activity with IC50 values of 3.4–37.8 µM. Compound 8 with a 2-mercaptoquinazolinone cap moiety displayed the highest antiproliferative efficacy against MCF-7 cells. For the HDAC6 target selectivity study, compound 8 displayed an IC50 value of 2.3 µM, which is 29.3 times higher than those of HDAC3, HDAC4, HDAC8, and HDAC11. Western blot assay proved that compound 8 strongly inhibited tubulin acetylation, a substrate of HDAC6. Compound 8 also displayed stronger inhibition activity against HDAC11 than the control drug Belinostat. The inhibitory mechanism of action of compound 8 on HDAC enzymes was then explored using molecular docking study. The data revealed a high binding affinity (−7.92 kcal/mol) of compound 8 toward HDAC6. In addition, dock pose analysis also proved that compound 8 might serve as a potent inhibitor of HDAC11.
Noninvasive and precise diagnosis of hepatic fibrosis is very important for the preventive therapeutic regimen of hepatic cirrhosis and cancer. In this study, we fabricated T 1 contrast Mn-porphyrin (MnTPPS 4 )/retinoic acid-chitosan ionic-complex nanoparticles (MRC NPs). The functional properties of MRC NPs were evaluated via transmission electron microscopy (TEM) imaging, release study, cytotoxicity assay, hepatocyte-specific uptake assay, and magnetic resonance (MR) imaging study. TEM images confirmed the typical structure of an ionic-complex NPs with around 100-200 nm of diameter. MnTPPS 4 is released from MRC NPs for up to 24 hr in con-
The objective of this paper is to assess the impact of supply chain linkage on the performance of aluminum profiles enterprises in Northern Vietnam. After qualitative research results, the research team has discovered a new variable in the linkage model which is the Policy linkage. The study performs official quantitative research on 289 aluminum profiles in Northern Vietnam and the results were analyzed on SPSS 22 and Smart PLS 3.0 software. The results indicate that the links in the supply chain include: Supply linkage, customer linkage, policy linkage and internal linkage all contribute significantly to supply chain management efficiency. Moreover, the supply chain management efficiency had a positive effect on business performance of aluminum profiles in the northern region of Vietnam. Finally, the study gives solutions and recommendations to help aluminum bar enterprises shape the northern region of Vietnam to better link in the supply chain and improve business performance.
Histone deacetylases (HDACs) have proven to be promising targets for the development of anticancer drugs. In this work, we report the design and synthesis of a series of 19 novel...
The objective of the research was to assess the factors affecting the quality of social infrastructure projects in the industrial zones in Hanoi, Vietnam ver the period 2018-2019 by means of qualitative and quantitative research methods where the quantitative research was conducted by an independent survey agency to enhance the objectivity of data. Adopting PLS -SEM method of Smart PLS, 3.0, we analyzed data from 396 valid questionnaires and the results showed that materials, design, construction and Stakeholder had positively affected the quality of Social Infrastructure Projects (SIPs). In the meantime, the project size also played a moderate role on the quality of social infrastructure projects.
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