Home About us Contact
|
Home About us Contact | ||
|
|
||
Cytotoxicity Studies (cytotoxicity + studies)
Selected AbstractsSynthesis and Cytotoxicity Studies of Fluorinated Derivatives of Vanadocene YEUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Issue 19 2009Brendan Gleeson Abstract From the reaction of 6-(2-fluoro-4-methoxyphenyl)fulvene (1a), 6-(3-fluoro-4-methoxyphenyl)fulvene (1b) and 6-[4-(trifluoromethoxy)phenyl]fulvene (1c) with LiBEt3H, lithiated cyclopentadienide intermediates (2a,c) were synthesised. These intermediates were then transmetallated to vanadium with VCl4 to yield the benzyl-substituted vanadocenes bis[(2-fluoro-4-methoxybenzyl)cyclopentadienyl]vanadium(IV) dichloride (3a), bis[(3-fluoro-4-methoxybenzyl)cyclopentadienyl]vanadium(IV) dichloride (3b), and bis[(4-trifluoromethoxybenzyl)cyclopentadienyl]vanadium(IV) dichloride (3c). The three vanadocenes 3a,c were characterised by single-crystal X-ray diffraction. All three vanadocenes had their cytotoxicity investigated through MTT-based preliminary in-vitro testing on the LLC-PK and Caki-1 cell lines in order to determine their IC50 values. Vanadocenes 3a,c were found to have IC50 values of 6.0 (+/,4), 35 (+/,7) and 13 (+/,3) ,M on the LLC-PK cell line and IC50 values of 78 (+/,11), 18 (+/,16) and 2.2 (+/,0.5) ,M on the Caki-1 cell line respectively. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009) [source] Synthesis of 2-Fluoro N10 -Substituted Acridones and Their Cytotoxicity Studies in Sensitive and Resistant Cancer Cell Lines and Their DNA Intercalation StudiesARCHIV DER PHARMAZIE, Issue 11 2009Yergeri C. Mayur Abstract A series of 2-fluoro N10 -substituted acridone derivatives with varying alkyl side chain length with propyl, butyl substitution, and a tertiary amine group at the terminal end of the alkyl side chain were synthesized and screened against cancer cell lines SW 1573, SW 1573 2R 160 (P-gp substrate) which are non-small lung cancer cell lines, MCF-7, MCF-7/MR (BCRP substrate) are breast cancer cell lines, 2008 WT, 2008MRP1, 2008MRP2, 2008MRP3 are ovarian cancer cell lines, and human embryo kidney cell lines like HEK293, HEK293 MRP4, and HEK293 MRP5i. The propyl-series compounds showed lipophilicity in the range of 1.93 to 4.40 and the butyl series in the range of 2.37 to 4.78. The compounds 4, 7, and 8 showed good cytotoxicity against the 60 human cancer cell line panel of the National Cancer Institute, USA. The compounds 14 and 15 showed a better cytotoxicity in most of the cancer cell lines compared to other compounds tested. The DNA-binding properties of the compounds were evaluated based on their affinity or intercalation with CT-DNA measured with absorption titration. The compound 11 bearing planar tricyclic ring linked with a butyl methylpiperazino side chain showed the highest binding affinity with a binding constant (Ki) of 10.38×10 M,1. Evaluation of the compounds in cell lines with an overexpression of various multidrug resistance-related protein (MRP), P-glycoprotein (P-gp), or Breast Cancer Resistance Protein (BCRP) showed that all compounds are not substrates for any of these transporters. [source] Synthesis and Cytotoxicity Studies of New Cryptophycin AnaloguesARCHIV DER PHARMAZIE, Issue 10 2009Wen Lu Liu Abstract Two analogues of cryptophycin were synthesized and biologically evaluated for their in-vitro cytotoxicities against several solid tumors and leukemia cell lines. The results revealed that both analogues exhibited a broad range of cytotoxic activity with observed IC50 values in the ,M-range, and compound 4 was more effective than compound 3 in most assays studied. [source] Controlled size chitosan nanoparticles as an efficient, biocompatible oligonucleotides delivery systemJOURNAL OF APPLIED POLYMER SCIENCE, Issue 4 2010Romila Manchanda Abstract Polymeric nanoparticles of chitosan crosslinked with glutaraldehyde have been prepared using reverse micellar system. An optically clear solution was obtained on redispersing these nanoparticles in aqueous buffer. The nanoparticles were characterized for their size and surface morphology employing dynamic laser scattering (DLS) and transmission electron microscopy (TEM). The TEM images showed spherical particles with smooth surface and narrow size distribution of about 90 nm, which was also supported by DLS data. Size and morphology of the particles remains the same on redispersing the lyophilized powder of these nanoparticles in aqueous buffer. Further, these nanoparticles were loaded with different synthetic oligonucleotides (ODNs). In vitro pH dependent release of the adsorbed oligonucleotides from these nanoparticles was also studied. At basic pH the release of oligonucleotides was found higher as compared with neutral and acidic medium. Cytotoxicity studies done on HEK 293 cells reveals that oligonucleotide loaded nanoparticles have high cell viability of nearly 76,88% whereas those of lipofectamine was about 35%. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2010 [source] Antimicrotubular and cytotoxic activity of geiparvarin analogues, alone and in combination with paclitaxelCELL BIOCHEMISTRY AND FUNCTION, Issue 3 2001Antonella Miglietta Abstract Geiparvarin is an antiproliferative compound isolated from the leaves of Geijera parviflora, and may represent a new drug which targets tubulin. To better explore the potential use of this agent, we investigated the antimicrotubular and cytotoxic effects of new synthetic aromatic derivatives of geiparvarin. These drugs inhibited polymerization of microtubular protein, particularly when the assembly was induced by paclitaxel. The microtubular network organization of fibroblasts was altered more effectively by some drugs. Normal microtubule architecture completely disappeared when the cells were treated simultaneously with drugs and paclitaxel: microtubules depolymerized or were reorganized into bundles, in a similar but more disarrayed fashion than that observed after treatment with paclitaxel alone. Cytotoxicity studies showed a dose-dependent effect, whereas combined administration of drugs and paclitaxel increased cytotoxicity, more effectively in paclitaxel versus derivatives administration alone. Copyright © 2001 John Wiley & Sons, Ltd. [source] Solubilizing efficiency and in vitro cytotoxicity of Peptoad GJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 4 2010Radhakrishna K. Maroju Abstract A novel non-ionic surfactant, Peptoad G, is evaluated for its solubilizing capacity and cytotoxicity in order to explore its possible use in aqueous formulation of hydrophobic drugs. Solubility studies were carried out using ten model hydrophobic drugs, and cytotoxicity of the surfactant was evaluated in three different cell lines using the MTT assay. It was shown that peptoad G enhances the solubility of the ten model drugs to different extents, ranging from 20- to 1100-fold, which correlated with the number of hydrogen-bonding sites on the drug molecules. The in vitro cytotoxicity studies revealed comparable cytotoxicity of peptoad G to that of cremophor EL. The results suggest peptoad G possesses potential as an alternative to conventional solubilizers in hydrophobic drug formulations. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99: 2196,2198, 2010 [source] Synthesis and cytotoxicity studies of novel anion-exchanged Titanocene Y derivativesAPPLIED ORGANOMETALLIC CHEMISTRY, Issue 10 2010James Claffey Abstract Starting from the potential anticancer drug candidate Titanocene Y {bis -[(4-methoxybenzyl)cyclopentadienyl]titanium(IV) dichloride}, anion exchange experiments were performed using silver malonate (1a) or silver cyclobutane-1,1-malonate (1b) in order to yield bis-[(4-methoxy-benzyl)cyclopentadienyl] titanium(IV) malonate (2a) and bis-[(4-methoxy-benzyl)cyclopentadienyl] titanium(IV) cyclobutane-1,1-malonate (2b). In addition, Titanocene Y was reacted with salicylic acid (3a) or 3,5-dinitro-salicylic acid (3b) in the presence of diethylamine to synthesize bis-[(4-methoxy-benzyl)cyclopentadienyl] titanium(IV) salicylate (4a) or bis-[(4-methoxy-benzyl)cyclopentadienyl] titanium(IV) 3,5-dinitro-salicylate (4b). These titanocenes had their cytotoxicity investigated through preliminary in vitro testing on the LLC-PK (pig kidney epithelial) cell line in an MTT-based assay in order to determine their IC50 values. Titanocenes 2a,b and 4a were found to have IC50 values of 74 ( ± 13) µM, 18 ( ± 5) µM and 49 ( ± 11) µM on the LLC-PK cell line, while compound 4b was found to have lost all its cytotoxic activity on this cell line. Copyright © 2010 John Wiley & Sons, Ltd. [source] | ||||||||||