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- Akbas, Esvet, et al.
(författare)
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Synthesis and Biological Evaluation of Novel Benzylidene Thiazolo Pyrimidin-3(5H)-One Derivatives
- 2024
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Ingår i: Polycyclic aromatic compounds (Print). - : Informa UK Limited. - 1040-6638 .- 1563-5333. ; 44:5, s. 3061-3078
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Tidskriftsartikel (refereegranskat)abstract
- Starting compound 1 was synthesized according to reference. 1 Benzylidene thiazole pyrimidin-3(5H)-ones were synthesized reactions of 1 with bromoacetic acid and various aryl-aldehydes in the same vessel via one-step, unlike studies in the literature. Quantum chemical parameters and full geometry optimizations for all compounds were computed using DFT based on B3LYP. Cytotoxic action potential of synthesized compounds was evaluated using trypan blue dye exclusion and MTT assays in different cell lines including adenocarcinoma alveolar basal epithelial-like adherent A549 cells, the colon adenocarcinoma HT-29 cells, prostate adenocarcinoma DU-145 cells, and diploid ARPE-19 retinal pigment epithelial cells. Embryotoxicity and genotoxicity assessments were performed on pluripotent human embryonal carcinoma NT2 and human lymphocyte cells, respectively. Compound A1 exhibited good anticancer activity on A549 and DU-145 cell lines, and the compounds including A3, 4, 6, and 9 induced cytotoxicity on A549 cells. The compounds A1-10 also showed a good biosafety profile at relatively lower concentrations.
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| 2. |
- Akbas, Esvet, et al.
(författare)
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Synthesis, Characterization, Theoretical Studies and in Vitro Embriyotoxic, Genotoxic and Anticancer Effects of Novel Phenyl(1,4,6-Triphenyl-2-Thioxo-1,2,3,4-Tetrahydropyrimidin-5-yl)Methanone
- 2023
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Ingår i: Polycyclic aromatic compounds (Print). - : Informa UK Limited. - 1040-6638 .- 1563-5333. ; , s. 1-18
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Tidskriftsartikel (refereegranskat)abstract
- In this study, phenyl (1,4,6-triphenyl-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methanone was obtained by using the Biginelli reaction method. The structure of this compound was analyzed using elemental analysis, IR, 1H, and 13C NMR. The quantum chemical calculations (QCC) of this compound were performed density functional theory (DFT) method, 6–31 G (d, p) base set, and B3LYP functions with the Gaussian09W software package. Literature shows that pyrimidine-derived compounds have very active biological properties. For this reason, the biologically active properties of the synthesized compound were also examined. To determine embryotoxic, genotoxic, and cytotoxic effects of compound, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT), lactate dehydrogenase (LDH) release, micronucleus (MN) and 8-OH-dG assays were carried out. On the other hand, pharmacokinetic and toxicity properties (ADMET) were predicted in silico via SwissADME and Protox-II web tools. In silico estimates of this compound used in the study showed that the compound has the covetable physicochemical properties for bioavailability. In conclusion, the obtained results of our study clearly showed that this compound exerted strong toxicity potential.
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| 6. |
- Manzetti, Sergio
(författare)
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Polycyclic Aromatic Hydrocarbons in the Environment : Environmental Fate and Transformation
- 2013
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Ingår i: Polycyclic aromatic compounds (Print). - : Informa UK Limited. - 1040-6638 .- 1563-5333. ; 33:4, s. 311-330
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Tidskriftsartikel (refereegranskat)abstract
- Polycyclic aromatic hydrocarbons are toxic and carcinogenic compounds that occur in the environment and derive from two classes processes: petrogenic and pyrogenic processes. The petrogenic part derives from oil- and drilling activities, including oil disasters, spills, and pollution from industrial sites, refineries, and most importantly traffic exhaust emissions, while the pyrogenic part derives from fires, forest fires, volcanic eruptions, and incineration. PAHs have long degradation periods, and recent studies show high accumulated concentrations in soil, aquatic, and atmospheric environments. Particularly with the advent of the winter season, pollution and pollution migration increases by the atmospheric influences on smog clouds, from air to soil, air to water reserves, and from air to humans. This review maps the recent measurements and concentrations of PAHs worldwide, with particular focus on highly exposed regions such as China, India and former Eastern European countries. Monitoring and mapping the fate of PAH is of particular value to environmental scientists, given the carcinogenic and toxic properties of several PAHs. As also reported in this review, the carcinogenicity and toxicity varies with the chemical and molecular character of PAHs varies with size and shape, and the carcinogenic and toxic effect can be higher according to season, type of fuel and source of pollution, and also by the size of the exposed region/site. PAHs are an ubiquitous pollutant class that has to be included in climate regulations at the same level with CO2 and NOx, given their longer half-life and chemical properties which gives a wide range of toxic derivatives during degradation.
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| 7. |
- Marchand, Charlotte, et al.
(författare)
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Physicochemical and Ecotoxicological Characterization of Petroleum Hydrocarbons and Trace Elements Contaminated Soil
- 2020
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Ingår i: Polycyclic aromatic compounds (Print). - : Taylor & Francis. - 1040-6638 .- 1563-5333. ; 40:4, s. 967-978
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Tidskriftsartikel (refereegranskat)abstract
- Underground storage tanks used for auto oil spill waste contain many hazardous materials, including polycyclic aromatic hydrocarbons (PAHs) trace elements. These compounds pose a significant threat to the environment and affect negatively human health. The aim of this study was to characterize the soil of a former auto scrap yards in which oil spill tank leakage occurred in Sweden. The soil samples were collected from an area of 5 m2 around an oil the tank which was highly contaminated with petroleum hydrocarbons (PHC) and trace elements (cobalt and lead). Another soil samples were collected from a nearby area that was not contaminated by PHC and they were considered as controls. The characterization of these soil samples was performed using two approaches. Analysis of the relevant physico-chemical soil properties included texture, organic matter, contaminant concentration and pH, while biological analyses were performed using three independent ecotoxicological tests with plant (Lepidium sativum), earthworm (Eisenia fetida) and soil microorganisms. Toxicity tests showed that contaminants had strongly negative effects on earthworm’s development and L. sativum shoots dry biomass in both PHC contaminated and control soils. These two parameters were the most sensitive in reflecting toxicity of study soils. Oxygen uptake rate (OUR) in aqueous phase was four times higher than that of the solid phase even though a similar trend was observed in both phases (aqueous and solid). Moreover, microorganism’s respiration was high in PHC contaminated soils in comparison to control soils due to the mineralization of readily available OM and/or organic pollutants as well as the inhibitory effect of TE on soil respiration. The results clearly demonstrated that combination of chemical analyses with three toxicity tests was appropriate to characterize mixed PHC and TE contaminated soils.
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