Anticancer activities of fatty acids and their heterocyclic derivatives

Traditional chemotherapy relies on the premise that rapidly proliferating cancer cells are more likely to be killed by a cytotoxic agent, but in reality, the long-standing problem of chemotherapy is the lack of tumor-specific treatments. Apart from the impact on tumor cells, the drugs’ major limitation is their severe adverse side effects on normal cells and tissues. Nutritional and epidemiological studies have indicated that cancer progression is correlated with the consumption of fatty acids, but the exact mechanisms still remain unknown. In the first part of our review, we discussed the beneficial effects of free fatty acids (saturated and unsaturated) on the progress of carcinogenesis in different tumor cell lines. We presented various mechanisms proposed in the literature, which explain the possible impact on the cells metabolism. The second part describes modifications of different fatty acids with existing anticancer drugs and heterocyclic moieties by condensation reactions. Such conjugations increased the tissue selectivity and made chemotherapy potentially more effective and less toxic in in vivo and in vitro studies. This fatty acid modifications, which change the activity of compounds, their uptake selectivity and alter drug delivery methods, may be the key to unlocking true medical potential of fatty acids

Electrochemical synthesis and structural studies of zinc(II) complexes with derivatives of benzo[b]furancarboxylic acids

Three novel zinc complexes with benzo[b]furan-carboxylic acids were obtained. The elemental and thermal analyses, and IR spectroscopy were used for basic characterization of compounds. The Zn(II) coordination geometry was studied by X-ray absorption spectroscopy. In microcrystalline powders for all complexes the cation is penta-coordinated (ZnO5) with the Zn–O distances equal to ca. 2 Å, as determined by extended X-ray absorption fine structure. For recrystallized Zn(II) complex 1 (with 7-acetyl-6-methoxy-3-methyl-benzo[b]furan-2-carboxylic acid) crystal structure was determined by X-ray crystallography, and this analysis indicated a distorted polyhedron around the cation in which one of the Zn–O distances is above 2.5 Å

The role of tumor-derived exosomes in tumor angiogenesis and tumor progression

Exosomes, belonging to the group of extracellular bodies, are released by healthy as well as cancerous cells and serve as a communication pathway. Tumor-derived exosomes (TEX) possess the capacity to reprogram the function of normal cells owing to their genetic and molecular cargo. Such exosomes target endothelial cells (among others) in the tumor microenvironment to promote angiogenesis. Blood supply is essential in solid tumor growth and metastasis. The potential of pro-angiogenic changes is enhanced by an increased amount of circulating tumor-derived exosomes in the body fluids of cancer patients. A vascular network is important, since the proliferation, as well as the metastatic spread of cancer cells depends on an adequate supply of oxygen and nutrients, and the removal of waste products. New blood vessels and lymphatic vessels are formed through processes called angiogenesis and lymphangiogenesis, respectively. Angiogenesis is regulated by both activator and inhibitor molecules. Thousands of patients have received anti-angiogenic therapy to date. Despite their theoretical efficacy, anti-angiogenic treatments have not proved beneficial in terms of long-term survival. Tumor-derived exosomes carrying pro-angiogenic factors might be a target for new anti-cancer therapy

Biological evaluation of novel 1,4-dithiine derivatives as potential antimicrobial agents

The preparation of twelve aminoalkanol derivatives of 2,3-dihydro-5H-[1,4] dithiino[2,3-c]pyrrole- 5,7(6H)-dione was described. Newly obtained compounds, as well as their propyl and butyl analogues, were evaluated in vitro against selected viruses. Selected derivatives were tested for their antibacterial and antifungal activity. Compounds 3h, 3j, 4b and 5a-d showed moderate to significant protections against CVB-2, HSV-1 and YFV viruses. The molecular structures of 4a, 5c and 5g were determined by an X-ray analysis

Antimicrobial activity of 10-(diphenylmethylene)-4-azatricyclo[5.2.1.0 2,6]dec-8-ene-3,5-dione derivatives

Antibacterial and antifungal activity of 10-(diphenylmethylene)-4- azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives were examined by the disk diffusion method (growth inhibition zone diameter in agar medium). The minimal inhibitory concentrations (MICs) for the most active agents were determined. Title compounds were also evaluated in vitro against HIV-1 virus and their cytotoxicity was determined. Aminoalkanol derivatives exhibited activity against the majority of microorganisms studied