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Wyniki wyszukiwania dla: ANTICANCER%20AGENTS
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Vitamin D and its analogs as anticancer and anti-inflammatory agents
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Selective Cytostatic and Cytotoxic Anticancer Effects of Bisfunctional Agents: A Strategy for the Design of DNA Binding Agents
PublikacjaVarious agents have been synthesized and proved useful for the National Cancer Institute's anticancer testing as potential new drugs, but most agents suffer side effects from their limited selectivity against cancer cells over healthy ones. Therefore, this paper attempts to describe drugs in terms of the level of tumor cell selectivity which they possess to define the features of mols. that are essential for useful cytotoxicity....
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Synthesis of conjugates of amino-combretastatin with tuftsin derivatives as potential anticancer agents
PublikacjaOpisano syntezę nowych koniugatów 3'-N-(tuftsyno lub retro-tuftsyno)-amino-kombretastatyny jako potencjalnych związków przeciw-nowotworowych. Do syntezy amino-kombretastatyny (amino-CA-4) wykorzystano reakację Wittiga a koniugatów metodę DPPA. Mamy nadzieję, że połączenie pochodnych tuftsyny z amino-CA-4 wpłynie na polepszenie właściwości terapeutycznych CA-4.
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Synthesis of conjugates of Combretastatin A-4 with tuftsin derivatives as potential anticancer agents
PublikacjaZaprezentowano syntezę nowych koniugatów Combretastatyny A-4 z pochodnymi tuftsyny i retro-tuftsyny, jako potencjalnych związków przeciwnowotworowych.
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Synthesis and Biological Evaluation of Acridine/Acridone Analogs as Potential Anticancer Agents
PublikacjaAcridine and acridone analogues were prepared by Ullmann condensation and then cyclization reaction. As a result of nucleophilic substitution reaction 1-nitro-9-phenoxyacridine or 1-chloro-4-nitro-9(10H)-acridone with the corresponding peptides, the planned acridine derivatives (10a-c, 12, 17-a-d, 19) have been obtained. The cytotoxic activity of the newly obtained analogs were evaluated against melanotic (Ma) and amelanotic (Ab)...
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In Search of Panacea—Review of Recent Studies Concerning Nature-Derived Anticancer Agents
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Ruthenium(II) and Iridium(III) Complexes as Tested Materials for New Anticancer Agents
PublikacjaThe oncological use of cisplatin is hindered by its severe side eects and a very important resistance problem. To overcome these problems, scientists have attempted to design new generation transition-metal anticancer complexes. In this study, we present new complexes, ruthenium(II) [(6-p-cymene)RuCl(py2CO)]PF6 (1), iridium(III) [(5-Cp)IrCl(py2CO)]PF6 (2), and NH4[IrCl4(py2CO)]H2O (3), based on di-2-pyridylketone (py2CO). The prepared...
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Sonochemical synthesis of rosuvastatin based novel 3-methyleneisoindolin-1-one derivatives as potential anticancer agents
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Chloroacridine derivatives as potential anticancer agents which may act as tricarboxylic acid cycle enzyme inhibitors
PublikacjaThe chloroacridines affect biological forms of melanoma in different ways. Amelanotic (Ab) melanoma (with inhibited melanogenesis and higher malignancy) was particularly sensitive to the action of the chloroacridines. The Ab melanoma cells died through apoptosis and through death without caspase activation. Diminished activity of TAC enzymes was noticed among Ab melanoma cells together with ATP/NAD depletion, especially in the...
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Synthesis of new antrapyridazone derivatives - a novel group of anticancer agents active on a multidrugresistant(MDR) tumor cell lines
PublikacjaNovel antrapyridazone derivatives were synthesized and biologically evaluated in order tobroaden the data on structure-activity relationship of this class of cytostatics. Recent literaturedata prove that acetamides react better with aryl chlorides. A new approach based onintroduction of other amides form into aromatic ring in Ullmann was tested. This new methodcould give better yields and make purification step more convenient.
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Rosuvastatin based novel 3-substituted isocoumarins / 3-alkylidenephthalides: Ultrasound assisted synthesis and identification of new anticancer agents
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Furanocoumarins in anticancer therapy – For and against
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Synthesis of 7-oxo-7h-naphto[1,2,3-de]quinoline derivatives as potential anticancer agents active on multidrug resistant cell lines
PublikacjaOpierając się na naszym wcześniejszym stwierdzeniu, że tetracykliczne analogi antrachinonów z wbudowanym pierścieniem pirydynowym wykazują aktywną cytotoksyczność względem komórek z indukowaną opornością, przeprowadzono syntezę pochodnych 7-oxo-7h-nafto[1,2,3-de]chinoliny (3, 6-8, 10-12, 14,15 i 18) posiadających jeden lub dwa zasadowe łańcuchy boczne i różne podstawniki w pierścieniu pirydynowym, związków o potencjalnym działaniu...
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Adverse Renal Effects of Anticancer Immunotherapy: A Review
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Adverse Renal Effects of Anticancer Immunotherapy: A Review
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Novel 2-(2-alkylthiobenzenesulfonyl)-3-(phenylprop-2-ynylideneamino)guanidine derivatives as potent anticancer agents – Synthesis, molecular structure, QSAR studies and metabolic stability
PublikacjaA series of new 2-(2-alkylthiobenzenesulfonyl)-3-(phenylprop-2-ynylideneamino)guanidine derivatives have been synthesized and evaluated in vitro by MTT assays for their antiproliferative activity against cell lines of colon cancer HCT-116, cervical cancer HeLa and breast cancer MCF-7. The obtained results indicated that these compounds display prominent cytotoxic effect. The best anticancer properties have been observed for derivatives...
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Chemometric methods for determination of mechanisms of action of anticancer compounds
PublikacjaW 1990 amerykański Narodowy Instytut Raka (NCI) wprowadził szeroki test przesiewowy in vitro mający na celu poszukiwanie nowych związków przeciwnowotworowych. Test został wdrożony po przebadaniu 171 standardowych związków przeciwnowotworowych. Przedmiotem niniejszej pracy jest próba stworzenia reguł klasyfikacji związków standardowych ze względu na ich mechanizm działania przeciwnowotworowego na podstawie wyników z testu NCI. Potwierdzono...
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ANTICANCER RESEARCH
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Binding free energy of selected anticancer compounds to DNA - theoreticalcalculations
PublikacjaPraca dotyczy swobodnej energii wiązania z DNA trzech związków o działaniu przeciwnowotworowym (mitoksantronu i dwóch pochodnych pirymidoakrydyny). Obliczenia wykorzystywały metody Poissona-Boltzmanna (udział elektrostatyczny) i metody SASA (udział nieelektrostatyczny). W wyniku badań zaproponowano struktury kompleksów jakie tworzą badane ligandy z DNA.
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Anticancer Properties of Amino Acid and Peptide Derivatives of Mycophenolic Acid
PublikacjaBackground: Although Mycophenolic Acid (MPA) is applied as prodrugs in clinic as an immunosuppressant, it also possesses anticancer activity. MPA acts as Inosine-5’-Monophosphate Dehydrogenase (IMPDH) inhibitor, where the carboxylic group at the end of the side chain interacts with Ser 276 of the enzyme via hydrogen bonds. Therefore, MPA derivatives with other polar groups indicated high inhibition too. On the other hand, potent...
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Design, synthesis, and biological evaluation of tetrahydroquinolinones and tetrahydroquinolines with anticancer activity
PublikacjaColorectal cancer (CRC) is the most commonly diagnosed cancer in Europe and the United States and the second leading cause of cancer related mortality. A therapeutic strategy used for the treatment of CRC involves targeting the intracellular levels of reactive oxygen species (ROS). In this study, we synthesized a series of novel tetrahydroquinolinones and assessed their ability to inhibit CRC growth and proliferation by evoking...
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Synthesis and biological evaluation of 2,7-Dihydro-3H-dibenzo[de,h]cinnoli- ne-3,7-done derivatives a novel group of anticancer agents active on a multidrug resistance cell line.
PublikacjaZsyntezowano serię pochodnych pirydazonu z jednym lub dwoma łańcuchami bocznymi w różnych pozycjach chromoforu tetracyklicznego. Związki wykazały aktywność cytoksyczną na mysią białaczkę L1210 i ludzką k562 oraz na linii komórkowej oporności krzyżowej MDR (k562/DX). Dwa najbardziej aktywne związki przetestowano in vivo na mysiej białaczce P388. Wykazały one aktywność przeciwnowotworową porównywalną z aktywnością Mitoxantronu.
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Effect of brefeldin A and castanospermine on resistant cell lines as supplements in anticancer therapy
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Liposomal Nanoformulation as a Carrier for Curcumin and pEGCG—Study on Stability and Anticancer Potential
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Quantitative proteomic analysis of anticancer drug RH1 resistance in liver carcinoma
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Anticancer Study on IrIII and RhIII Half-Sandwich Complexes with the Bipyridylsulfonamide Ligand
PublikacjaTwo non-platinum compounds, organometallic half-sandwich complexes [(η 5 -Cp)IrCl(L)]PF 6 (1) and [(η 5 -Cp)RhCl(L)]PF 6 (2) were prepared by treating pentamethylcyclopentadienyl chloride dimers of iridium(III) or rhodium(III) with the obtained 4-amino-N-(2,2'-bipyridin-5- yl)benzenesulfonamide ligand (L) and ammonium hexafluorophosphate. The crystal structures of ligand (L) and complexes 1 and 2 were obtained and then analyzed. Coordination...
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Single-wall carbon nanotubes based anticancer drug delivery system
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Study of the anticancer potential of Cd complexes of selenazoyl-hydrazones and their sulfur isosters
PublikacjaThe biological activity of Cd compounds has been investigated scarce since Cd has been recognized as a human carcinogen. However, the toxicity of cadmium is comparable to the toxicity of noble metals such as Pt and Pd. The paradigm of metal toxicity has been challenged suggesting that metal toxicity is not a constant property, yet it depends on many factors like the presence of appropriate ligands. Studies on anticancer activity...
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ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
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Anticancer properties of low molecular weight oat beta-glucan – An in vitro study
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<p>Analysis of toxicity and anticancer activity of micelles of sodium alginate-curcumin</p>
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Methods for Elucidation of DNA-Anticancer Drug Interactions and Their Applications in the Development of New Drugs
PublikacjaDNA damaging agents including anthracyclines, camptothecins and platinum drugs are among most frequently used drugs in the chemotherapeutic routine. Due to their relatively low selectivity for cancer cells, administration is associated with adverse side effects, whereas the inherent genotoxicity of these drugs is associated with risk of developing secondary cancers. Development of new drugs, which could be spared of these drawbacks...
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Synthesis of 5-arylidene-2-amino-4-azolones and evaluation of their anticancer activity
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Synthesis and Anticancer Activity of Mitotic-Specific 3,4-Dihydropyridine-2(1H)-thiones
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Batracylina (BAT) - potencjalny lek przeciwnowotworowy. Batracylin (BAT) - potential of anticancer drug
PublikacjaOpisano działanie potencjalnego leku przeciwnowotworowego - batracyliny(BAT). Batracylina została wyselekcjonowana przez National Cancer Institute (NCI, Bethesda, USA) w 1978 roku jako efekt programu poszukiwań nowych leków chemioterapii.Związek ten w badaniach in vivo u myszy okazał się bardzo aktywny przeciw nowotworowi okrężnicy 38 (colon 38), trudnemu do wyleczenia przez znane leki przeciwnowotworowe. Okazała się ona skuteczna...
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New Chalcone Derivatives Containing 2,4-Dichlorobenzenesulfonamide Moiety with Anticancer and Antioxidant Properties
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Structural, physicochemical and anticancer study of Zn complexes with pyridyl-based thiazolyl-hydrazones
PublikacjaThiazolyl-hydrazones (THs) exhibit a wide spectrum of biological activity that can be enhanced by complexation with various metal ions. Zn(II) complexes with α-pyridine-1,3-TH ligands may represent an alternative to the standard platinum-based chemotherapeutics. In addition, they show photoluminescence properties and thus can be regarded as multifunctional materials. In this study, we synthesized and characterized three neutral...
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Amygdalin: Toxicity, Anticancer Activity and Analytical Procedures for Its Determination in Plant Seeds
PublikacjaAmygdalin (D-Mandelonitrile 6-O--D-glucosido--D-glucoside) is a natural cyanogenic glycoside occurring in the seeds of some edible plants, such as bitter almonds and peaches. It is a medically interesting but controversial compound as it has anticancer activity on one hand and can be toxic via enzymatic degradation and production of hydrogen cyanide on the other hand. Despite numerous contributions on cancer cell lines, the clinical...
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Anticancer properties of ester derivatives of betulin in human metastatic melanoma cells (Me-45)
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Synthesis and Characterization of Size- and Charge-Tunable Silver Nanoparticles for Selective Anticancer and Antibacterial Treatment
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An In Vitro Antimicrobial, Anticancer and Antioxidant Activity of N–[(2–Arylmethylthio)phenylsulfonyl]cinnamamide Derivatives
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Cisplatin filled multiwalled carbon nanotubes – a novel molecular hybrid of anticancer drug container
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The covalent and non-covalent conjugation of graphene oxide with hydroxycamptothecin in hyperthermia for its anticancer activity
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Novel N-(aryl/heteroaryl)-2-chlorobenzenesulfonamide derivatives: synthesis and anticancer activity evaluation
PublikacjaA new series of N-(aryl/heteroaryl)-2-chlorobenzenesulfonamide derivatives 4-21 have been synthesized, and evaluated at the National Cancer Institute (USA) for their in vitro activities against a panel of 60 different human cancer cell lines. Among them, compounds 16, 20 and 21 exhibited remarkable cytotoxic activity against numerous human cancer cell lines. We found that sulfonamide derivative 21 appeared to be more selective...
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Synthesis, structure, DNA binding and anticancer activity of mixed ligand ruthenium(II) complex
PublikacjaIn order to obtain a potential chemotherapeutic which is not affected on the normal BALB/3T3 cell line, a new arene ruthenium(II) complex {[RuCl(L1)(η6-p-cymene)]PF6}2 · H2O has been synthesized by a direct reaction of precursor, [{(η6-p-cymene)Ru(μ-Cl)}2Cl2], with N,N-chelating ligand (L1 - 2,2′-bis(4,5-dimethylimidazole). The compound has been fully characterized by elemental analysis, X-ray diffraction, IR, UV–Vis and 1H, 13C...
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Metallochromic azole azomacrocyclic reagents
PublikacjaW artykule opisano syntezę makrocyklicznych azozwiązków zawierających resztę pirolową lub imidazolową. Zbadano zdolność kompleksowania jonów metali w acetonitrylu (spektroskopia UV-Vis). Otrzymane związki przetestowano jako jonofory w membranowych elektrodach jonoselektywnych.
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Non-enzymatic glutathione-mediated conjugation of unsymmetrical bisacridine C-2028 with anticancer activity
Dane BadawczeThe presented data complement the studies on the interplay between C-2028 (anticancer-active unsymmetrical bisacridine) and the glutathione S-transferase/glutathione (GST/GSH) system.
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Synthesis, Molecular Structure, Metabolic Stability and QSAR Studies of a Novel Series of Anticancer N-Acylbenzenesulfonamides
PublikacjaA series of novel N-acyl-4-chloro-5-methyl-2-(R1-methylthio)benzenesulfonamides 18–47 have been synthesized by the reaction of N-[4-chloro-5-methyl-2-(R1-methylthio) benzenesulfonyl]cyanamide potassium salts with appropriate carboxylic acids. Some of them showed anticancer activity toward the human cancer cell lines MCF-7, HCT-116 and HeLa, with the growth percentages (GPs) in the range from 7% to 46%. Quantitative structure-activity relationship...
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Chemical composition, antioxidant and anticancer effects of the seeds and leaves and indigo (polygonum tinctorium Ait.) Plant
PublikacjaSeeds and leaves of indigo (Polygonum tinctorium Ait.) plant were investigated and compared with another medicinal plant named prolipid for their properties such as chemical composition, antioxidant, and anticancer effects by Fourier transform infrared, three-dimensional fluorescence spectroscopy, and electrospray ionization-MS in negative mode. It was found that polyphenols, flavonoids, and flavanols were significantly higher...
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Molecular basis for the DNA damage induction and anticancer activity of asymmetrically substituted anthrapyridazone PDZ-7
Publikacjanthrapyridazones, imino analogues of anthraquinone, constitute a family of compounds with remarkable anti-cancer activity. To date, over 20 derivatives were studied, of which most displayed nanomolar cytotoxicity towards broad spectrum of cancer cells, including breast, prostate and leukemic ones. BS-154, the most potent derivative, had IC50 values close to 1 nM, however, it was toxic in animal studies. Here, we characterize another...