The aim of the present study was to investigate antiproliferative and proapoptotic actions N-(5-benzyl-1,3-thiazol-2-yl)-3,5-dimethyl-1-benzofuran-2-carboxamide derivative (compound 5) in glioma cells comparison with temozolomide (TMZ) doxorubicin (Dox), used as positive controls. activity compound 5, TMZ, Dox on human glioblastoma U251 multiform T98G measured using MTT test. Western blot analysis, fluorescent microscopy, agarose gel retardation assay, flow cytometric DNA comet assay under...

Aim.To determine the in vitro effect of thiazole derivative and its complex with polyethylene glycol (PEG)-based nanoscale particles on ROS generation NK/Ly lymphoma cells hepatocytes mice.Methods.The effects BF-1 (N-(5-benzyl-1,3-thiazol-2-yl)-3,5-dimethyl-1-benzofuran-2-carboxamide), PEG-based polymeric nanoparticles (Th1, Th3, Th5) their complexes (Th2, Th4, Th6) production murine were studied using fluorescent microscopy.The level superoxide both was determined a spectrophotometric...

The influence of newly synthesized thiazole derivative N-(5-benzyl-1,3-thiazol-2-yl)-3,5-dimethyl-1-benzofuran-2-carboxamide on cellular ultrastructure and anti­oxidant system activity in lymphoma cells was studied vitro . A pronounced cytotoxic action the tumor reported earlier. However, no cytotoxicity this substance detected toward non-cancerous cells. In addition, it shown that scavengers active forms Oxygen significantly reduced a effect compound. It found derivatives at concentrations...

Background. A pronounced cytotoxic action of the thiazole derivatives complexed with polymeric carriers on tumor cells in vitro was reported earlier, while no cytotoxicity these compounds detected toward noncancerous cells. It found that at concentrations 10 and 50 µM affected lymphoma cell ultrastructure vitro. The purpose this work to investigate effect derivative 8-methyl-2-Me-7-[trifluoromethyl-phenylmethyl]-pyrazolo-[4,3-e]-[1,3]- thiazolo-[3,2-a]-pyrimidin-4(2H)-one (PP2) its complexes...

The development of a new anticancer drugs targeted at energy metabolism tumor cells is promising­ approach for cancer treatment. aim our study was to investigate the action thiazole derivative N-(5-benzyl-1,3-thiazol-2-yl)-3,5-dimethyl-1-benzofuran-2-carboxamide (BF1) and its complex with PEG based polymeric nanoparticle (PEG-PN) on respiration mitochondrial membrane potential in murine NK/Ly cells. rate oxygen uptake recorded by polarographic method using Clark electrode. relative values...

Background. Previous studies have shown a pronounced cytotoxic effect of thiazole derivatives in combination with polymeric carriers on tumor cells. At the same time, were not against non-cancerous cells vitro. It was that at concentrations 10 and 50 μM affected prooxidant antioxidant systems lymphoma The aim this work to study complex derivative N-(5-benzyl-1,3-thiazol-2-yl)-3,5-dimethyl-1-benzofuran-2-carboxamide (BF1) poly(VEP-co-GMA)-graft-mPEG (Th1), poly(PEGMA) (Th3) poly(PEGMA-co-DMM)...

Many chemotherapeutics drugs have low water solubility, which potentially can decrease their anticancer potential. The use of drug delivery systems has proven to be highly effective in addressing the challenges associated with delivering hydrophobic chemotherapy tumor tissues. However, two major issues that arise clinical nanoparticle-based treatment cancer are hepatotoxicity and suppression hematopoietic system, limit medical applicability. As previously established, thiazole derivative...

Background. Our previous studies have shown a minor embryotoxic effect of polymeric poly(VEP-co-GMA)-graft-mPEG carrier on Missgurnus fossilis L. embryos and prelarvae. At the same time, it was found that 3-day exposure to 10-15 M polymer slowed developing, which is characterized by delayed hatching larvae. However, in 10-day experiment loach larvae exposed carrier, anomalies defects development not been identified. The aim this work analyze prelarvae survival, as well determine morphometric...

Background. Mitochondria can influence cancer cells both indirectly via reactive oxygen species mediation and directly through mitochondrial biogenesis. Energy production in mitochondria is crucial as it facilitates the synthesis of essential molecules needed for cellular biosynthesis, growth, proliferation. The development new anticancer drugs that target energy metabolism tumor shows promise treatment. Our study aimed to investigate how thiazole derivative...

Previous in vitro studies have demonstrated a pronounced cytotoxic effect of the thiazole derivative N-(5-Benzyl-13-thiazole-2-yl)-35-dimethyl-1-benzofuran-2-carboxami­de (BF1) on tumor cells. Additionally, it has been determined that scavengers reactive Oxygen species (ROS) significantly reduce BF1. In this study, influence BF1 activity superoxide dismutase (SOD) and catalase (CAT), both normally presence ascorbic acid, mouse Nemeth-Kellner lymphoma (NK/Ly) cells studied to evaluate...

One of the main problems chemotherapy is development negative side effects, when anti-tumor drugs damage healthy cells, in particular hepatocytes. Liver detoxifying organ human and animals. This plays an important role excretion from body. Changes free radical oxidation processes respiratory function mitochondria liver cells following effects newly synthesized antitumor agents may indicate adverse that often occur after taking such substances. It was shown thiazole derivatives passess...

Background. Many types of tumors are sensitive to changes in prooxidant-antioxidant balance. Thus, further studies on reactive oxygen species inducing antitumor drugs that generate oxidative stress-dependent cytotoxic effects promising. Our previous works showed thiazole derivatives combination with polymeric carriers have a pronounced effect tumor, while not being against pseudo-normal cells vitro. It was found complex PEG-based affected the antioxidant system lymphoma The aim this work...

Background. The influence in vitro of thiazole derivative 8-methyl-2-Me-7-[trifluoro­methyl-phenylmethyl]-pyrazolo-[4,3-e]-[1,3]-thiazolo-[3,2-a]-pyrimidin-4(2H)-one (PP2) on the level lipid peroxidation products, superoxide anion radical and antioxidant system activity lymphoma cells was studied. A pronounced cytotoxic action tumor reported earlier, however, no cytotoxicity this substance detected toward non-cancerous cells. In addition, it shown that sca­vengers active forms Oxygen...

Thiazole derivatives were shown to have toxic effects in vitro on cancer cells of different origin and can be considered as potentially antineoplastic, but their effect the normal tissues needs studied.In this research newly synthesized thiazole 3] thiazolo [3, pyrimidin-4 (2H)-one (PP2) used pro-and antioxidant processes after adding a 1, 10 50 μM concentrations liver homogenate healthy NK/Ly lymphoma-bearing mice was estimated.the level superoxide radical tBa-active products well catalase,...

Background. Drug delivery systems (DDS) have demonstrated a significant ability to overcome many of the challenges associated with hydrophobic chemotherapeutic compounds tumor tissues. However, hepatotoxicity and suppression hematopoietic system are key problems in clinical treatment cancer by nanoparticle-based DDS that can limit their medical exposure. The aim this work was investigate effect thiazole derivative N-(5-benzyl-1,3-thiazol-2-yl)-3,5-dimethyl-1-benzofuran-2-carboxamide (BF1)...

Хіміотерапія, хоч і залишається лікуванням першої лінії, проте має багато недоліків, які зумовлюють зниження ефективності протипухлинних препаратів, включаючи системні побічні ефекти; низьку проникність в пухлину; неселективність дії лікарських препаратів; резистентність пухлинних клітин до багатьох хіміопрепаратів; недостатню розчинність та стабільність засобів, тощо [1]. Відомо, що хіміотерапевтичних препаратів спричиняють неспецифічну гепатотоксичність, яка визнана обмежуючим фактором у...

Background. The search for optimal methods of selective and integral determination various cytotoxic compounds in biological fluids tissues, which would have high sensitivity allow quick reliable assessment detection potentially components substances with biologically active action, remains relevant today. It is known that chemotherapeutic agents can be released into the environment (air, surface water, sediments soil) cause adverse consequences (impact on stability ecosystems due to reduced...