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Published in Anton Sebastian, A Dictionary of the History of Medicine, 2018
Aniline An extract from coal tar used as a dye, and later recognized as a cause of methemoglobinemia. Its precursor, nitrobenzene, was found to be carcinogenic. Robert Koch (1843–1910) used aniline dyes for microscopic staining in 1877. See bladder carcinoma.
Nitrogen compounds
Published in Bev-Lorraine True, Robert H. Dreisbach, Dreisbach’s HANDBOOK of POISONING, 2001
Bev-Lorraine True, Robert H. Dreisbach
Ingestion of 1 g of aniline has caused death, although recovery has followed ingestion of 30 g. The toxicity of nitrobenzene is similar. The fatal dose (LD50) in animals for aniline is 400 mg/kg, and for nitrobenzene it is 700 mg/kg. The toxicities of aniline derivatives are given in Table 9.1. Infant deaths have been caused by absorption of aniline from diapers stenciled with cloth-marking ink containing aniline as the vehicle for dyes. The residual pigment is safe after washing.
Green-Synthesized Nanoparticles as Potential Sensors for Health Hazardous Compounds
Published in Richard L. K. Glover, Daniel Nyanganyura, Rofhiwa Bridget Mulaudzi, Maluta Steven Mufamadi, Green Synthesis in Nanomedicine and Human Health, 2021
Rachel Fanelwa Ajayi, Sphamandla Nqunqa, Yonela Mgwili, Siphokazi Tshoko, Nokwanda Ngema, Germana Lyimo, Tessia Rakgotho, Ndzumbululo Ndou, Razia Adam
One additional hazardous chemical to human health is nitrobenzene (Fig. 13.2), a toxic nitroaromatic compound used in the production of many commercially appropriate chemicals. Commercially, nitrobenzene and its derivatives are widely used in the manufacturing of dyes, explosives, perfumes, pesticides and pharmaceuticals. Conversely, the growth of these industries produces a large quantity of wastewater comprising of nitrobenzene, which brings toxicological inferences to human health such as anaemia, cancer and skin irritation (Li et al., 2020). Additionally, when inhaled, nitrobenzene is carcinogenic in humans and presents with symptoms such a cyanosis, dizziness, nausea, restlessness and vomiting. Other studies (e.g. Villegas et al., 2020) have reported additional symptoms such as a burning sensation in the mouth and throat, coordination disorders, a smell of bitter almonds in the exhaled air, signs of paralysis, tachycardia, a drop in blood pressure and unconsciousness. Despite its carcinogenic and toxic nature, the USEPA has certified nitrobenzene as group 2B carcinogen and has detailed a minimum threshold limit of 5 ppb for humans. Furthermore, nitrobenzene groundwater aquifer and soil pollution have become a serious issue resulting from its toxicity and potential harmful health impacts on humans. This is caused by the fact that these compounds are resistant to oxidative degradation resultant from the stability of the benzene rings and effects of the electron-withdrawing nitro groups making its quantification and detection a priority in most countries (Liu et al., 2020). Structure of nitrobenzene.
Development of reliable quantitative structure–toxicity relationship models for toxicity prediction of benzene derivatives using semiempirical descriptors
Published in Toxicology Mechanisms and Methods, 2023
Ayushi Singh, Sunil Kumar, Archana Kapoor, Parvin Kumar, Ashwani Kumar
Nitroaromatics are toxic compounds that cause skin hypersensitivity, immunotoxicity, germ cell degeneration, inhibition of liver enzymes, and perhaps carcinogenicity. The lack of experimental data made modeling the toxicity of nitroaromatic chemicals difficult. Nitrobenzenes (NBs) are commonly utilized as industrial chemicals and, as a result, have a significant potential for contamination (Zoeteman et al. 1980). NBs are significant fine organic intermediates that are employed in a variety of applications, including medicine, dye, and explosive synthesis (Wang et al. 2014). The majority of NBs and their derivatives are hazardous and has a significant risk of polluting the environment. NBs are escaping into the environment at an alarming rate with the advancement of agricultural and industrial rates (Artemenko et al. 2011). They are reactive substances that have been reported to be oxidative phosphorylation uncouplers and may be considered pro-electrophiles that produce potentially very hazardous C-nitroso compounds. The toxicity of NBs has been extensively studied due to their ubiquitous use, and they have been the focus of a number of QSAR investigations. The NBs are electrophilic toxicants in that they can undergo a variety of electrophilic reactions depending on their substitution pattern. The toxicity of NBs has been thoroughly investigated by multiple groups of researchers using various approaches (Roberts 1987; Bellifa and Mekelleche 2016).
Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Abdallah E. Abdallah, Reda R. Mabrouk, Maged Mohammed Saleh Al Ward, Sally I. Eissa, Eslam B. Elkaeed, Ahmed B. M. Mehany, Mariam A. Abo-Saif, Ola A. El-Feky, Mohamed S. Alesawy, Mohamed Ayman El-Zahabi
The docking results revealed the ability of the new derivatives to accommodate VEGFR-2 pocket and form interactions in a mode similar to that of sorafenib. These results are not only consistent with biological data obtained from the VEGFR-2 assay but also give an explanation to them. For example, quinazoline based derivatives (14a,b and 15a–d) displayed the best docking energy (from –53.63 to –66.52 C-Docker energy score) as presented in Table 6. Regarding VEGFR-2 inhibition, the same derivatives were the most potent (IC50 ranged from 60 to 94.22 nM) as listed in Table 1. The most potent candidates for VEGFR-2 inhibition were 15d and 15c with IC50 = 60.00 and 65.24 nM, respectively. Similarly, these two compounds were the most promising in terms of docking score showed the highest binding free energies 64.11 and 66.52 C-Docker energy score, respectively. At the same time, quinoxaline-based derivatives (19a,b and 20a–d) came the second with regard to both VEGFR-2 inhibition and docking score as illustrated in Tables 1 and 6. It can also be seen that nitrobenzene-based derivatives came last in both biological activity and docking results.
Small Molecule Inhibitors of Programmed Cell Death Ligand 1 (PD-L1): A Patent Review (2019–2021)
Published in Expert Opinion on Therapeutic Patents, 2022
Jingjing Deng, Zhengqi Cheng, Juyang Long, Alexander Dömling, Micky Tortorella, Yuanze Wang
Later, chemists from Shanghai Institute of Materia Medica (Chinese Academy of Sciences) described 156 1,3-dihydroxy phenyl derivatives. (Figure 3) [24] In this series of compounds different types of soluble groups were used, for example, sulfonic acids and polyalcohols were introduced for the tail group. One of the most potent molecules, 2 exhibited an IC50 of 0.88 nM in the in vitro PD-1/PD-L1 binding assay. Meanwhile, in an efficacy experiment at a concentration of 40 mg/kg, 2 was able to significantly inhibit tumor growth in a melanoma model. In another patent, the Shanghai Institute of Organic Chemistry (Chinese Academy of Sciences) disclosed 106 compounds with similar structures [25]. In an HTRF binding assay, at a dose of 1 μΜ, compound 3 showed 99.94% inhibition of PD-1/PD-L1 interaction. China Pharmaceutical University has filed a patent with 49 molecules that use nitrobenzene as the aryl moiety [26]. 4 displayed an IC50 of 2.7 nM in blocking the binding of the PD-1/PD-L1 interaction in vitro without any cytotoxicity against Lewis lung carcinoma (LLC) cells. In addition, 4 was able to dose-dependently elevate interferon-γ production and counteract PD-1/PD-L1 induced immunosuppression.