Triggered by the resounding success of cisplatin, the past decades have seen tremendous efforts to produce clinically beneficial analogues. The recent achievement of oxaliplatin for the treatment of colon cancer should, however, not belie the imbalance between a plethora of investigated complexes and a very small number of clinically approved platinum drugs. Strategies opening up new avenues are increasingly being sought using complexes of metals other than platinum such as ruthenium or gallium. Based on the chemical differences between these metals, the spectrum of molecular mechanisms of action and potential indications can be broadened substantially. Other approaches focus on complexes with tumour-targeting properties, thereby maximizing the impact on cancer cells and minimizing the problem of adverse side effects, and complexes with biologically active ligands.

Antitumour metal compounds: more than theme and variations

Translation into Russian:  Tomasetti, C. , Li, L. , & Vogelstein, B.  (2017).  Stem cell divisions, somatic mutations, cancer etiology, and cancer prevention . Science ,  355 (6331), 1330-1334. DOI:  10.1126/science.aaf9011

Stem cell divisions, somatic mutations, cancer etiology, and cancer prevention

Thiazoles, their benzofused systems, and thiazolidinone derivatives are widely recognized as nuclei of great value for obtaining molecules with various biological activities, including analgesic, anti-inflammatory, anti-HIV, antidiabetic, antitumor, and antimicrobial. In particular, in the past decade, many compounds bearing these heterocycles have been studied for their promising antibacterial properties due to their action on different microbial targets. Here we assess the recent development of this class of compounds to address mechanisms underlying antibiotic resistance at both bacterial-cell and community levels (biofilms). We also explore the SAR and the prospective clinical application of thiazole and its benzofused derivatives, which act as inhibitors of mechanisms underlying antibiotic resistance in the treatment of severe drug-resistant infections. In addition, we examined all bacterial targets involved in their antimicrobial activity reporting, when described, their spontaneous frequencies of resistance.

Thiazoles, Their Benzofused Systems, and Thiazolidinone Derivatives: Versatile and Promising Tools to Combat Antibiotic Resistance

An overview on the recent developments of 1,2,4-triazine derivatives as anticancer compounds

Derivatives of pyridine and thiazole hybrid: Synthesis, DFT, biological evaluation via antimicrobial and DNA cleavage activity.

Synthesis and Antimicrobial Activity of Some Novel bis Polyfunctional Pyridine, Pyran, and Thiazole Derivatives

The inhibitory effect of three newly synthesized hydrazide derivatives on carbon steel corrosion in hydrochloric acid showed better inhibition efficiency (97.5%) and their inhibition mechanism is presented.

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Experimental and surface morphological studies of corrosion inhibition on carbon steel in HCl solution using some new hydrazide derivatives

Synthesis and Anti-inflammatory Evaluation of Some New Pyrazole, Pyrimidine, Pyrazolo[1,5-a]Pyrimidine, Imidazo[1,2-b]Pyrazole and Pyrazolo[5,1-b]Quinazoline Derivatives Containing Indane Moiety

Corrosion of carbon steel is a major problem that destroys assists of industries and world steel installations; the importance of this work is to introduce new heterocyclic compounds as effective and low-cost corrosion inhibitors. Three compounds of carbohydrazide derivatives, namely: 5-amino-N′-((2-methoxynaphthalen-1-yl)methylene)isoxazole-4-carbohydrazide (H4), 2,4-diamino-N′-((2-methoxy-naphthalene-1-yl)methylene) pyrimidine-5-carbohydrazide (H5) and N′-((2-methoxynaphthalen-1-yl)methylene)-7,7-dimethyl-2,5-dioxo-4a,5,6,7,8,8a-hexahydro-2H-chromene-3-carbohydrazide (H6) were used to examine the efficacy of corrosion of carbon steel in 1 M hydrochloric acid solution. This corrosion efficacy was detected by utilizing various methods including electrochemical impedance spectroscopy (EIS), potentiodynamic polarization (PDP), weight loss measurements (WL), surface morphology analyses by atomic force microscopy (AFM), quantum chemical computations based on density functional theory (DFT) and molecular dynamics (MD) simulation. The results indicated that these compounds act as mixed type inhibitors i.e. reduce the corrosion rate of carbon steel due to the formation of a stable protective film on the metal surface and reduce the cathodic hydrogen evolution reaction. As confirmed from impedance, carbohydrazide derivatives molecules are adsorbed physically on metal surface with higher corrosion efficacy reached to (81.5–95.2%) at 20 × 10−6 M concentration at room temperature. Temkin isotherm model is the most acceptable one to describe the carbohydrazide derivative molecules adsorption on the surface of carbon steel. Protection mechanism was supported by quantum chemical analyses and Monte Carlo modeling techniques. The theoretical calculations support the experimental results obtained. This proves the use of carbohydrazide derivatives as a very effective inhibitors against the corrosion of carbon steel in acidic media.

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Effectiveness of some novel heterocyclic compounds as corrosion inhibitors for carbon steel in 1 M HCl using practical and theoretical methods

A novel series of N-1 arylidene amino imidazole-2-thiones were synthesized, identified using IR, 1H-NMR, and 13C-NMR spectral data. Cytotoxic effect of the prepared compounds was carried out utilizing three cancer cell lines; MCF-7 breast cancer, HepG2 liver cancer, and HCT-116 colon cancer cell lines. Imidazole derivative 5 was the most potent of all against three cell lines. DNA flow cytometric analysis showed that, imidazoles 4d and 5 exhibit pre-G1 apoptosis and cell cycle arrest at G2/M phase. The results of the VEGFR-2 and B-Raf kinase inhibition assay revealed that compounds 4d and 5 displayed good inhibitory activity compared with reference drug erlotinib.

https://www.mdpi.com/1420-3049/26/6/1706/pdf

Elsherbiny H. El-Sayed

Papers

Synthesis and Antimicrobial Activity of Some Novel bis Polyfunctional Pyridine, Pyran, and Thiazole Derivatives

Experimental and surface morphological studies of corrosion inhibition on carbon steel in HCl solution using some new hydrazide derivatives

Synthesis and Anti-inflammatory Evaluation of Some New Pyrazole, Pyrimidine, Pyrazolo[1,5-a]Pyrimidine, Imidazo[1,2-b]Pyrazole and Pyrazolo[5,1-b]Quinazoline Derivatives Containing Indane Moiety

Effectiveness of some novel heterocyclic compounds as corrosion inhibitors for carbon steel in 1 M HCl using practical and theoretical methods

5-Aryl-1-Arylideneamino-1H-Imidazole-2(3H)-Thiones: Synthesis and In Vitro Anticancer Evaluation.