Synthesis and anticancer activities of diquinazoline diselenides compounds

A series of novel diquinazoline diselenide compounds was designed and synthesized with substituted 4-chloroquinazoline and sodium diselenide. Their structures were confirmed by IR, 1H NMR, 13C NMR, and elemental analyses.The antitumor activity of the new compounds was evaluated by MTT method. Compound 1a, 1c, 1h and 1i were found to have activities against MDA-MB-435, A549,MDA-MB-231, SiHa, and HeLa cells. Moreover, compared with the commercial anticancer drugs Gefitinib, Oxaliplatin,Taxol, 10-Hydroxycamptothec in, and Epirubicin Hydrochloride,1a exerted better antitumor effects on corresponding cell lines at 10 μM

Antimicrobial Activity of Quinazolin Derivatives of 1,2-Di(quinazolin-4-yl)diselane against Mycobacteria

Mycobacterium tuberculosis (M. tuberculosis) is one of the leading causes of morbidity and mortality. Currently, the emergence of drug resistance has an urgent need for new drugs. In previous study, we found that 1,2-di(quinazolin-4-yl)diselane (DQYD), a quinazoline derivative, has anticancer activities against many cancers. However, whether DQYD has the activity of antimycobacterium is still little known. Here our results show that DQYD has a similar value of the minimum inhibitory concentration with clinical drugs against mycobacteria and also has the ability of bacteriostatic activity with dose-dependent and time-dependent manner. Furthermore, the activities of DQYD against M. tuberculosis are associated with intracellular ATP homeostasis. Meanwhile, mycobacterium DNA damage level was increased after DQYD treatment. But there was no correlation between survival of mycobacteria in the presence of DQYD and intercellular reactive oxygen species. This study enlightens the possible benefits of quinazoline derivatives as potential antimycobacterium compounds and furtherly suggests a new strategy to develop new methods for searching antituberculosis drugs

Water quality characteristics and source analysis of pollutants in the Maotiao river basin (SW China)

Rivers are an important mediator between human activities and the natural environment. They provide multiple functions, including irrigation, transportation, food supply, recreation, and water supply. Therefore, evaluations of water quality and pollution sources are of great significance for ecological restoration and management of rivers. In this study, the improved “vušekriterijumska optimizacija i kompromisno rješenje” (VIKOR in Serbianin English: Multicriteria Optimization and Compromise Solution), and a geodetector were used to analyze the water quality characteristics and pollution sources of the Maotiao River Basin (Gizhou province, SW China). The results showed that the water quality of the Maotiao River Basin deteriorated significantly during the summer drought period, as was evident in the reservoirs and lakes. It improved in the wet season (i.e., during the summer period) due to runoff dilution. Water quality decreased along the river’s course, from upstream to downstream sections. The results of the geographic detector analysis showed that agricultural areas were the primary factor affecting the spatial distribution of water quality in the river basin. In July, August, and November 2020, the influence of agricultural land was 0.72, 0.60, or 0.80, respectively, and the interactions among urban, industrial, agricultural, and forested areas explained 99.2%, 83.2%, or 99.9% of the spatial differentiation of water quality, respectively. Due to the influence of spatial scale, settlements have a small influence on the spatial distribution of water quality. Their impact factors were 0.38, −0.24, and −0.05, respectively. Notably, the negative relationship of water quality and forested areas reflects that topography, types of landscapes, and soil thickness have considerable influences on the Maotiao River Basin’s water quality. Based on the findings, we infer that good farmland water conservancy projects and comprehensive management of different types of landscapes, such as forests, agriculture, and urban area and water bodies, are of great significance for improving water quality