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Cytotoxic Activity (cytotoxic + activity)
Kinds of Cytotoxic Activity Selected AbstractsCorrigendum: Antimicrobial, Hemolytic, and Cytotoxic Activities of ,-Peptoid,Peptide Hybrid Oligomers: Improved Properties Compared to Natural AMPsCHEMBIOCHEM, Issue 12 2010Christian A. Olsen Dr. No abstract is available for this article. [source] ChemInform Abstract: Phytochemical Constituents from the Flowers of Gymnaster koraiensis and Their Cytotoxic Activities in vitroCHEMINFORM, Issue 22 2010Il Kyun Lee Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Green Chemoselective Synthesis of Thiazolo[3,2-a]pyridine Derivatives and Evaluation of Their Antioxidant and Cytotoxic Activities.CHEMINFORM, Issue 8 2010Feng Shi Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Synthesis of Novel Quinoxaline Derivatives and Its Cytotoxic Activities.CHEMINFORM, Issue 48 2009Shinji Tanimori Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Short Approach Towards New Isocoumarins and Dihydroisocoumarins and Investigation of Their Cytotoxic Activities.CHEMINFORM, Issue 30 2009Isolde Wetzel Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Novel Diterpenoids with Potent Inhibitory Activity Against Endothelium Cell HMEC and Cytotoxic Activities from a Well-Known TCM Plant Daphne genkwa.CHEMINFORM, Issue 24 2005Zha-Jun Zhan Abstract For Abstract see ChemInform Abstract in Full Text. [source] Syntheses, in vitro Antibacterial and Cytotoxic Activities of a Series of 3-Substituted Succinimides.CHEMINFORM, Issue 13 2005Frederic Zentz Abstract For Abstract see ChemInform Abstract in Full Text. [source] ChemInform Abstract: Design, Synthesis, Photochemical Properties and Cytotoxic Activities of Water-Soluble Caged L-Leucyl-L-leucine Methyl Esters that Control Apoptosis of Immune Cells.CHEMINFORM, Issue 20 2002Hironori Mizuta Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Antitumor-Promoting Effects and Cytotoxic Activities of Dammar Resin Triterpenoids and Their DerivativesCHEMISTRY & BIODIVERSITY, Issue 8 2010Motohiko Ukiya Abstract Nineteen known triterpenoids, 1,19, and one known sesquiterpenoid, 20, were isolated from dammar resin obtained from Shorea javanica K. & V. (Dipterocarpaceae). One of the acidic triterpenoids, dammarenolic acid (1), was converted to fourteen derivatives, namely, an alcohol, 21, an aldehyde, 22, and twelve L -amino acid conjugates, 23,34. Compounds 1,34 were examined for their inhibitory effects on the induction of Epstein,Barr virus early antigen (EBV-EA) by 12- O -tetradecanoylphorbol 13-acetate (TPA) in Raji cells, a known primary screening test for antitumor promoters. All of the compounds tested, except for compounds 4, 5, 12,14, 16, and 17, showed inhibitory effects against EBV-EA activation with potencies either comparable with or stronger than that of , -carotene, a known natural antitumor promoter. In addition, (20S)-20-hydroxy-3,4-secodammara-4(28),24-dien-3-al (22) exhibited inhibitory effects on skin tumor promotion in an in vivo two-stage mouse skin carcinogenesis test based on 7,12-dimethylbenz[a]anthracene (DMBA) as initiator, and with TPA as promoter. Furthermore, evaluation of the cytotoxic activities of compounds 1,34 against human cancer cell lines showed that reduction (i.e., 21 and 22) or conjugation with L -amino acids (i.e., 23,34) of compound 1 enhanced the cytotoxicity against human melanoma cell line CRL1579. [source] Antimicrobial and Cytotoxic Activities of Neolignans from Magnolia officinalisCHEMISTRY & BIODIVERSITY, Issue 3 2004Wan-Jr Syu In the light of the steady increase of infections related to vancomycin-resistant enterococci (VRE) and methicillin-resistant Staphylococcus aureus (MRSA), the medicinal plant Magnolia officinalis was subjected to bioassay-directed fractionation, which led to the isolation of the known neolignans piperitylmagnolol (1), magnolol (2), and honokiol (3) from the MeOH extract. In broth-microdilution assays, 1,3 exhibited antibacterial activities against VRE and MRSA at minimum-inhibitory concentrations (MIC) in the range of 6.25,25,,g/ml, compound 1 being the most-potent antibiotic. The ratio of MBC/MIC (MBC=minimum bactericidal concentration) was ,2 for all compounds. The kinetics of the antibacterial action of 1 and 3 were studied by means of time-kill assays; both compounds were bactericidal against VRE and MRSA, their actions being time dependent, or both time and concentration dependent. Magnolol (2) was acetylated to magnolol monoacetate (4) and magnolol diacetate (5) (partial or full masking of the phenolic OH functions). The cytotoxic properties of 1,5 against human OVCAR-3 (ovarian adenocarcinoma), HepG2 (hepatocellular carcinoma), and HeLa (cervical epitheloid carcinoma) cell lines were evaluated. The CD50 values for compounds 1,3 were in the range of 3.3,13.3,,g/ml, derivatives 4 and 5 being much less potent. This study indicates that piperitylmagnolol (=3-[(1S,6S)-6-isopropyl-3-methylcyclohex-2-enyl]-5,5,-di(prop-2-enyl)[1,1,-biphenyl]-2,2,-diol; 1) possesses both significant anti-VRE activity and moderate cytotoxicity against the above cancer cell lines. [source] Platinum(IV) Complexes of 3- and 4-Picolinic Acids Containing Ammine or Isopropylamine Ligands , Synthesis, Characterization, X-ray Structures, and Evaluation of Their Cytotoxic Activity against Cancer Cell Lines,EUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Issue 30 2008María J. Macazaga Abstract The preparation and characterization of the new complexes trans -[PtCl4(NH3)(3-picolinic acid)] (1), trans -[PtCl4{NH2CH(CH3)2}(3-picolinic acid)] (2), trans -[PtCl4(NH3)(4-picolinic acid)] (3), and trans -[PtCl4{NH2CH(CH3)2}(4-picolinic acid)] (4) are described. The main structural feature of these complexes is the presence of ligands capable of multiple hydrogen-bonding interactions. Crystals of 1, 2, 3, and 4 suitable for single-crystal X-ray diffraction were grown, and the molecular structures of these compounds are discussed. In contrast to the inactive parent PtII complexes, the PtIV complexes displayed cytotoxic activity against various cancer cell lines used at the National Cancer Institute (NCI) for in vitro screens. Once more, the isopropylamine derivatives showed the best cytotoxicity values. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008) [source] Characterization by NMR Spectroscopy, X-ray Analysis and Cytotoxic Activity of the Ruthenium(II) Compounds [RuL3](PF6)2(L = 2-Phenylazopyridine or o -Tolylazopyridine) and [RuL'2L"](PF6)2(L', L" = 2-Phenylazopyridine, 2,2'-Bipyridine)EUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Issue 13 2005Anna C. G. Hotze Abstract Tris(ligand) complexes [RuL3](PF6)2 (L = 2-phenylazopyridine or o -tolylazopyridine) and mixed ligand [RuL'2L"](PF6)2 (L' and L" are 2-phenylazopyridine or 2,2'-bipyridine) have been synthesized, structurally characterized and investigated for cytotoxic activity. These complexes are important to study the hypothesis that the compound ,-[Ru(azpy)2Cl2] (azpy = 2-phenylazopyridine) exhibits a high cytotoxicity due to its two cis chloride ligands, which might be exchanged for biological targets as DNA. Molecular structures of mer -[Ru(azpy)3](PF6)2 (1) and mer -[Ru(tazpy)3](PF6)2 (5) (tazpy = o -tolylazopyridine) have been determined by X-ray diffraction. Series of complexes [RuL3](PF6)2 and [RuL'2L"](PF6)2 show interesting NMR spectroscopic data; e.g. the spectrum of mer -[Ru(azpy)3](PF6)2 (1) shows extremely broadened resonances at room temp. but sharpened resonances at low temperature. In the 1H NMR spectra of compounds [Ru(azpy)2(bpy)]2+ and [Ru(bpy)2(azpy)]2+ (bpy = 2,2-bipyridine), respectively, less broadened (room temp.) or completely sharp resonances (room temp.) occur in comparison to 1 (under same conditions). By selecting the right temperature and/or concentration, NMR spectra of these series of compounds have been resolved using 2D COSY and NOESY NMR spectroscopy. Remarkably, the cytotoxicity data against a series of human tumor cell lines (A498, EVSA-T, H226, IGROV, M19, MCF-7 and WIDR) show a moderate cytotoxicity for these series of tris(ligand) complexes. So, even though no chloride ligands are present in these tris(ligand) complexes, a considerable cytotoxic activity is observed. This would imply that the 2-phenylazopyridine ruthenium(II) complexes act by a completely different mechanism than the well-known cisplatin. This finding is important, because an anticancer compound acting via a different mechanism is a prerequisite in designing new anticancer drugs. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005) [source] Synthesis and Cytotoxic Activity of Novel Amidine Analogues of Bis(2-chloroethyl)amineARCHIV DER PHARMAZIE, Issue 8 2009Krzysztof Bielawski Abstract Novel nitrogen mustard agents 7,12 involving 4-(N,N -bis(2-chloroethyl)aminophenyl)propylamine linked to a 5-(4- N -alkylamidinophenyl)-2-furancarboxylic acid moiety by the formation of an amide bond have been synthesized, characterized, and evaluated for their in-vitro cytotoxic activity against MDA-MB-231 and MCF-7 human breast cancer cells. Evaluation of the cytotoxicity of 7,12 employing a MTT assay and inhibition of [3H]thymidine incorporation into DNA demonstrated that these compounds exhibit remarkable cytotoxic effects in comparison with 4-[bis(2-chloroethyl)amino]benzenebutanoic acid. Compounds 7 and 9, which possess a cationic amidine and 4,5-dihydro-1H -imidazol function moiety are approximately ten times more potent than 4-[bis(2-chloroethyl)amino]benzenebutanoic acid. The new compounds were evaluated as DNA topoisomerase II inhibitors. The cytotoxicity of the compounds 7,12 correlates with their DNA-binding affinities and their relative potency as topoisomerase II inhibitors. [source] ChemInform Abstract: Regiospecific Microwave-Assisted Synthesis and Cytotoxic Activity Against Human Breast Cancer Cells of (RS)-6-Substituted-7- or 9-(2,3-dihydro-5H-1,4-benzodioxepin-3-yl)-7H- or -9H-purines.CHEMINFORM, Issue 50 2008Ana Conejo-Garcia Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Synthesis of 5,6-Dimethyl-9-methoxy-1-phenyl-6H-pyrido[4,3-b]carbazole Derivatives and Their Cytotoxic Activity.CHEMINFORM, Issue 12 2006Ryszard Jasztold-Howorko Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Cytotoxic Activity of Nepetin, a Flavonoid from Eupatorium ballotaefolium HBK.CHEMINFORM, Issue 16 2005G. C. G. Militao Abstract For Abstract see ChemInform Abstract in Full Text. [source] Contortisiliosides A-G: Isolation of Seven New Triterpene Bisdesmosides from Enterolobium contortisiliquum and Their Cytotoxic Activity.CHEMINFORM, Issue 28 2004Yoshihiro Mimaki No abstract is available for this article. [source] Isolation, Structural Elucidation, and Synthesis of RA-XVII, a Novel Bicyclic Hexapeptide from Rubia cordifolia, and the Effect of Side Chain at Residue 1 upon the Conformation and Cytotoxic Activity.CHEMINFORM, Issue 21 2004Yukio Hitotsuyanagi No abstract is available for this article. [source] Synthesis and Cytotoxic Activity of A-Ring Modified Betulinic Acid Derivatives.CHEMINFORM, Issue 52 2003Young-Jae You Abstract For Abstract see ChemInform Abstract in Full Text. [source] Synthesis and Cytotoxic Activity of 1,3-Benzodioxole Derivatives.CHEMINFORM, Issue 36 2003Part 2. Abstract For Abstract see ChemInform Abstract in Full Text. [source] Norlanostane and Lanostane Glycosides from the Bulbs of Chionodoxa luciliae and Their Cytotoxic Activity.CHEMINFORM, Issue 24 2003Kazutomo Ori Abstract For Abstract see ChemInform Abstract in Full Text. [source] Synthesis and Cytotoxic Activity of Pyridazinol[1,,6,:1,2]pyrido[3,4-b]indol-5-inium Derivatives as Anticancer Agents.CHEMINFORM, Issue 6 2003Julio Alvarez-Builla Abstract For Abstract see ChemInform Abstract in Full Text. [source] ChemInform Abstract: Design and Synthesis of Some New Pyranoxanthenone Aminoderivatives with Cytotoxic Activity.CHEMINFORM, Issue 36 2002George Kolokythas Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Synthesis and Cytotoxic Activity of Benzophenanthrolinone Analogues of Acronycine.CHEMINFORM, Issue 6 2002Jean-Bernard Bongui Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Synthesis and Cytotoxic Activity of 2-Dialkylaminoethylamino Substituted Xanthenone and Thioxanthenone Derivatives.CHEMINFORM, Issue 2 2001Ioannis Kostakis Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Synthesis, DNA-Binding, Cleavage, and Cytotoxic Activity of New 1,7-Dioxa-4,10-diazacyclododecane Artificial Receptors Containing Bisguanidinoethyl or Diaminoethyl Double Side ArmsCHEMISTRY - A EUROPEAN JOURNAL, Issue 34 2007Xin Sheng Abstract Novel 1,7-dioxa-4,10-diazacyclododecane artificial receptors with two pendant aminoethyl (3) or guanidinoethyl (4) side arms have been synthesized. Spectroscopy, including fluorescence and CD spectroscopy, of the interactions of 3, 4, and their copper(II) complexes with calf thymus DNA indicated that the DNA binding affinity of these compounds follows the order Cu2+,4>Cu2+,3>4>3, and the binding constants of Cu2+,3 are Cu2+,4 are 7.2×104 and 8.7×104,M,1, respectively. Assessment by agarose gel electrophoresis of the plasmid pUC,19 DNA cleavage activity in the presence of the receptors showed that the complexes Cu2+,3 and Cu2+,4 exhibit powerful supercoiled DNA cleavage efficiency. Kinetic data of DNA cleavage promoted by Cu2+,3 and Cu2+,4 under physiological conditions fit to a saturation kinetic profile with kmax values of 0.865 and 0.596,h,1, respectively, which give about 108 -fold rate acceleration over uncatalyzed supercoiled DNA. This acceleration is due to efficient cooperative catalysis of the copper(II) center and the functional (diamino or bisguanidinium) groups. In-vitro cytotoxic activities toward murine melanoma B16 cells and human leukemia HL-60 cells were also examined: Cu2+,4 shows the highest activity with IC50 values of 1.62×10,4 and 1.19×10,5,M, respectively. [source] Two New Pregnanone Derivatives with Strong Cytotoxic Activity from Pachysandra axillarisCHEMISTRY & BIODIVERSITY, Issue 7 2005Ming-Hua Qiu Two new, bioactive, pregnane-based natural products, pachysanonin (=3,,11,,12,)-12-acetoxy-3-(dimethylamino)-11-[(3,4-dimethylpent-3-enoyl)oxy]pregnan-20-one; 1) and pachysanone (=(11,,12,)-12-acetoxy-11-[(3,4-dimethylpent-3-enoyl)oxy]pregnan-3,20-dion; 2) have been isolated from Pachysandra axillaris. Their structures were determined by spectroscopic methods, and, in the case of 2, by single-crystal X-ray crystallography (Figure). Compound 2 showed significant antitumor activity against Lewis lung carcinoma (LCC) tumor cells, with an IC50 value of 0.020±0.006,,g/ml, which is equal or even lower than those of the well-known natural antitumor agents harringtonine (0.02), homoharringtonine (0.15), and adriamycin (0.06,,g/ml; positive control). [source] Significant cytotoxic activity in vitro of the EGFR tyrosine kinase inhibitor gefitinib in acute myeloblastic leukaemiaEUROPEAN JOURNAL OF HAEMATOLOGY, Issue 5 2008Elin Lindhagen Abstract Objectives:, Gefitinib inhibits epidermal growth factor receptor (EGFR) signalling, but may also act by non-EGFR dependent mechanisms. We have investigated the activity of gefitinib in haematological tumour cells, in particular acute myeloblastic leukaemia (AML). Methods:, Cytotoxic activity of gefitinib, alone or in combination with standard anti-leukaemic drugs, was assessed by the short-term fluorometric microculture cytotoxicity assay in tumour cells from 117 patients representing five haematological and five non-haematological malignancies. In AML, the EGFR status was analysed by immunochemistry. Gefitinib-induced apoptosis was investigated in a subset of AML samples, as well as in the leukaemia cell line MV-4-11, using a multiparametric high content screening assay. To confirm activation of caspase-3 in cells treated with gefitinib, a blocking test was carried out in which MV4-11 cells were pretreated with the specific caspase inhibitor DEVD-FMK. Results:, Gefitinib showed highest cytotoxic activity in AML (n = 19) with many samples being sensitive at concentrations achievable in clinical practice (<10 ,M), and no difference between previously untreated and relapsed patients. No correlation between the activity of gefitinib and standard antileukaemic drugs (cytarabine, doxorubicin, etoposide) was observed. Combining gefitinib with these drugs resulted in mainly additive or synergistic (etoposide) effects, with no evidence of sequence dependency. The AML cells did not express the EGFR. Gefitinib induced apoptosis, which was at least partly mediated by activation of the caspase-3 pathway. Conclusion:,In vitro, gefitinib has significant cytotoxic activity in AML by inducing apoptosis through non-EGFR dependent pathways. [source] Synthesis of Polyamines from Ethylenediamine and Their Platinum(II) Complexes, Potential Antitumor AgentsEUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Issue 9 2006Mara Rubia Costa Couri Abstract This work describes the synthesis and characterization of five new amine ligands and also the preparation and characterization of their respective platinum(II) complexes by reaction with K2PtCl4 in water. These ligands were obtained by treatment of different halides or epoxides with ethylenediamine. Cytotoxic activity and cellular accumulation of three complexes were investigated in a human small-cell lung carcinoma cell line and its cisplatin resistant subline. The introduction of a spacer (cycle) between the two platinum atoms leads to a significant decrease in cytotoxic activity. At equitoxic doses, the intracellular platinum concentrations found for compounds 12 and 15 were significantly higher than those found for the reference compounds, cisplatin, carboplatin, or compound 9. This fact suggests that the formation of adducts between compounds 12 and 15 and the putative pharmacological target, DNA, is less favored. If these compounds bind more slowly to DNA, interaction with other intracellular ligands such as sulfur-containing molecules will become relevant and it may be the reason for the elevated intracellular platinum concentrations. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2006) [source] Cytotoxic T-cell responses to Mycobacterium bovis during experimental infection of cattle with bovine tuberculosisIMMUNOLOGY, Issue 2 2003Margot A. Skinner Summary Cytotoxic T-cell responses are thought to play a significant role in the host defence against mycobacterial infections. Little is understood about such responses of cattle to Mycobacterium bovis, the causative agent of bovine tuberculosis. The work described in this report demonstrates the activity of cytotoxic cells during experimental infection of cattle with M. bovis. The cytotoxic cells were found to have the ability to specifically lyse macrophages infected with M. bovis and were detected in peripheral blood lymphocytes after in vitro re-exposure to M. bovis. Cytotoxic activity was detected 4 weeks after experimental infection with M. bovis; a similar level of activity was maintained during the infection and it was mediated by both WC1+,, and CD8+ T cells. In addition, inhibition of the growth of M. bovis within infected macrophages was detected when they were exposed to cultures containing M. bovis -specific cytotoxic cells. The ability to detect cytotoxic cells after infection of cattle with M. bovis will allow their activity to be measured during vaccination trials. Correlation of cytotoxic activity with disease outcome may aid in the design of new vaccines and vaccination strategies. [source] | ||||||||||||||||||||||||||||||||||