Search results for "Amide"

On the Retention of Diuretics in Micellar Liquid Chromatography and Their Site of Action Within the Nephron

1993

Abstract The therapeutical action of diuretics has been attributed to their hydrophobic character, among other properties. Therapeutical and physiological classifications of diuretics are correlated. The site of action of high efficacay diuretics is the loop of Henle, that of intermediate efficacy diuretics is the distal tubule and that of low efficacy diuretics is the proximal and distal tubules, and the collecting duct. Partition coefficients between water and micelles offer a scale for hydrophobicity, which leads to a further correlation between retention in Micellar Liquid Chromatography (MLC), with a sodium dodecyl sulphate mobile phase and an ODS-C18 column, and the sites of action wi…

Sulfamide antifolates inhibiting thymidylate synthase: synthesis, enzyme inhibition and cytotoxicity

2002

Synthesis and biological evaluation are described of seven new analogues (3-9) of two potent thymidylate synthase inhibitors, 10-propargyl-5,8-dideazafolate (1) and its 2-methyl-2-deamino congener ICI 198583 (2). While the new compunds 3 and 4 were analogues of 1 and 2, respectively, containing a p-aminobenzenesulfonyl residue in place of the p-aminobenzoic acid residue, the remaining 5 new compounds were analogues of 4 with the L-glutamic acid residue replaced by glycine (5), L-valine (6), L-alanine (7), L-phenylglycine (8) or L-norvaline (9). The new analogues were tested as inhibitors of thymidylate synthases isolated from tumour (Ehrlich carcinoma), parasite (Hymenolepis diminuta) and n…

Mapping of the high molecular weight kininogen binding site of prekallikrein. Evidence for a discontinuous epitope formed by distinct segments of the…

1993

Prekallikrein, a glycoprotein involved in contact phase activation, circulates in plasma in the form of a binary complex with high molecular weight kininogen (H-kininogen). The binding to H-kininogen is mediated by the prekallikrein heavy chain consisting of four repetitive domains, A1-A4. To define more precisely the region(s) involved in kininogen binding, we have employed an affinity cross-linking strategy with a synthetic peptide of 31 residues which mimics the prekallikrein binding site of H-kininogen. Cross-linking of the radiolabeled peptide to (pre)kallikrein revealed a binding segment in the NH2-terminal portion of the prekallikrein heavy chain; another binding segment was located …

Nanodevices based on a novel galactosaminated phospholipid-polyaspartamide for liver targeting of a ribavirin prodrug

2011

Liver X Receptor ligand cytotoxicity in colon cancer cells and not in normal colon epithelial cells depends on LXRβ subcellular localization

2015

Increasing evidence indicates that Liver X Receptors (LXRs) have some anticancer properties. We recently demonstrated that LXR ligands induce colon cancer cell pyroptosis through an LXRβ-dependent pathway. In the present study, we showed that human colon cancer cell lines presented differential cytoplasmic localizations of LXRβ. This localization correlated with caspase-1 activation and cell death induction under treatment with LXR ligand. The association of LXRβ with the truncated form of RXRα (t-RXRα) was responsible for the sequestration of LXRβ in the cytoplasm in colon cancer cells. Moreover t-RXRα was not expressed in normal colon epithelial cells. These cells presented a predominantl…

Solvent-modulated structures in anilato-based 2D coordination polymers

2017

Abstract This work highlights the key role of the solvents in the structures of the series of 2D compounds [Ln2(C6O4Br2)3·(Solvent)n]·G (G = Guest). This study is based on the affinity and ability of these solvents to coordinate to lanthanides and on their possibility to act as solvation molecules. For this purpose here we focus on the Er(III) ion and on the bromanilato bridging ligand ([C6O4Br2]2− = dianion of 3,6-dibromo-2,5-dihydroxy-1,4-benzoquinone) and we play with three solvents: H2O, DMSO (dimethylsulfoxide) and DMF (dimethylformamide). Here we report the synthesis, crystal structure and magnetic characterization of compounds [Er2(C6O4Br2)3(H2O)6]·12H2O (1), [Er2(C6O4Br2)3(DMSO)4]·2…

Solvent-modulation of the structure and dimensionality in lanthanoid-anilato coordination polymers.

2018

We show the key role that the size and shape of the solvent molecules may play in the dimensionality and structure of a series of lanthanoid–chloranilato coordination polymers. We report the synthesis, structure and magnetic properties of six different coordination polymers prepared with Er(III) and chloranilato (C6O4Cl22− = 3,6-dichloro-2,5-dihydroxy-1,4-benzoquinone) and six different solvents: [Er2(C6O4Cl2)3(H2O)6]·10H2O (1), [Er2(C6O4Cl2)3(FMA)6]·4FMA·2H2O (2) (FMA = formamide = NH2CHO), [Er2(C6O4Cl2)3(DMSO)4]·2DMSO·2H2O (3) (DMSO = dimethy sulfoxide = Me2SO), [Er2(C6O4Cl2)3(DMF)6] (4) (DMF = dimethylformamide = Me2NCHO), [Er2(C6O4Cl2)3(DMA)4] (5) (DMA = dimethylacetamide = Me2NC(Me)O) …

Novel Lipophilic Lanthanide Bis-Phthalocyanines Functionalized by Pentadecylphenoxy Groups: Synthesis, Characterization and UV-Photostability

2012

Novel sandwich-type phthalocyanines containing a rare earth metal core (Pr, Nd, Eu-Lu) and macrocycles peripherally substituted by pentadecylphenoxy groups were synthesized using a cardanol-based phthalonitrile precursor and the respective lanthanide acetate. Additionally, the metal free-base analog compound was studied for comparison. The purified reaction products were all found to be thick and viscous substances at room temperature, showing liquid crystalline behavior with a distinct increase in fluidity at ca. 40 ° C. The complexes are readily soluble in chloroalkyl solvents and dissolve fairly well in DMF with some tendency to form aggregates. Besides they are strongly hydrophobic and …

Co-crystallization of Keggin type polyoxometalates [HL]3[PW12O40] and [Ln(DMF)8][PW12O40] (Ln=La, Dy, Yb) (L=N-(2-hydroxyphenyl)-3-methoxy-salicylide…

2016

Abstract Four new Keggin type polyoxometalate clusters [HL]3[PW12O40]·5MeOH (1) and [Ln(DMF)8][PW12O40] {Ln = La (2), Dy (3), Yb (4)} (L = N-(2-hydroxyphenyl)-3-methoxy-salicylideneamine) have been synthesized. Co-crystallization of complex 1 with each of the three complexes 2–4 takes place when the Schiff base ligand is treated with hydrated phosphotungstic acid, H3[PW12O40]·xH2O, hydrated lanthanide nitrate, Ln(NO3)3·6H2O in the presence of Ni(NO3)2·6H2O. The Schiff base ligand is protonated in complex 1 and thus it is neutralizing the charge of the polyoxotungstate anion, [PW12O40]3−. A dimethylformamide (DMF) coordinated trivalent lanthanide ion balances the negative charge of the polyo…

Short, full-dose adjuvant chemotherapy (CT) in high-risk adult soft tissue sarcomas (STS): long-term follow-up of a randomized clinical trial from th…

2016

[Background] To report on long-term results of a phase 3 trial comparing three versus five cycles of adjuvant chemotherapy (CT) with full-dose epirubicin+ifosfamide in high-risk soft tissue sarcomas (STS).