The nonestrogen receptor-mediated antiproliferative action of antiestrogen binding site (AEBS) ligands, including triphenylethylene antiestrogens and phenothiazines, has been linked to their ability to inhibit protein kinase C (PKC). Recent studies indicate that some diphenylmethane derivatives inhibit growth, are potent AEBS ligands, and antagonize histamine binding at an AEBS-related histamin...

BMY-28864 is a derivative of carbohydrate-binding antibiotic pradimicin A. This study aimed to examine the carbohydrate-binding specificity of BMY-28864 by a direct binding assay using neoglycolipids synthesized by conjugation of various oligosaccharides with dipalmitoylphosphatidylethanolamine (DPPE). Neoglycolipids were chromatographed on a thin layer chromatography plate and then subjected t...

Reaction of the mononuclear Ni(II) thiolate complexes [Ni(L)] [L, L(1), H2L(1), bis(2-mercaptoethyl)-1,2-dimercaptoethane; L(2), H2L(2), N,N'-dimethyl-N,N'-bis(2-mercaptoethyl)-bis(aminoethyl)sulfide] with [FeCp(CO)2I] gives the dithiolate-bridged heterobimetallic species, [Ni(L(1))FeCp(CO)]PF6, 1, and [Ni(L(2))FeCp]I, 2, respectively. Binding of a Fe(CO)3 fragment via reaction of square-planar...

BACKGROUND Antitumor cyclopalladated complexes with low toxicity to laboratory animals have shown leishmanicidal effect. These findings stimulated us to test the leishmanicidal property of one palladacycle compound called DPPE 1.2 on Leishmania (Leishmania) amazonensis, an agent of simple and diffuse forms of cutaneous leishmaniasis in the Amazon region, Brazil. METHODOLOGY/PRINCIPAL FINDINGS...

Palladacycle complex DPPE 1.2 was previously reported to inhibit the in vitro and in vivo infection by Leishmania (Leishmania) amazonensis. The aim of the present study was to compare the effect of DPPE 1.2, in association with heat-killed Propionibacterium acnes, on L. (L.) amazonensis infection in two mouse strains, BALB/c and C57BL/6, and to evaluate the immune responses of the treated anima...

BACKGROUND There is an urgent need to develop drug-loaded biocompatible nanoscale packages with improved therapeutic efficacy for effective clinical treatment. To address this need, a novel poly (2-hydroxyethyl methacrylate)-poly (lactide)-1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine [PHEMA-g-(PLA-DPPE)] copolymer was designed and synthesized to enable these nanoparticles to be pH responsiv...

The prevalence of asthma continues to increase in westernized countries, and optimal treatment remains a significant therapeutic challenge. Recently, CD1d-restricted invariant NKT (iNKT) cells were found to play a critical role in the induction of airway hyperreactivity (AHR) in animal models and are associated with asthma in humans. To test whether iNKT cell-targeted therapy could be used to t...

A nitrogen ligand, i.e. 1,3-di-(o-aminophenoxy)-2-propyl propargyl ether (DPPE), has been synthesized and characterized. Magnetic mesoporous silica composite (MNP@SiO2-SBA) was obtained via embedding magnetite nano-particles (MNPs) between SBA-15 channels. DPPE palladium dichloride (MNP@SiO2-SBA-DPPE-Pd(II)) then prepared click chemistry fully The Hiyama reaction conditions including solvent, a...

Described herein are preparations of synthetic models for the deactivated Ni(II)Fe(II) states of the [NiFe]-hydrogenases. Iodination of the S = ½ species [(dppe)Ni(pdt)Fe(CO)(3)](+) afforded the diamagnetic iodo complex [(dppe)Ni(pdt)IFe(CO)(3)](+). Crystallographic analysis of this species confirmed the presence of square-pyramidal Ni linked to an octahedral Fe centre. The NiFe separation of 3...

PURPOSE N,N-Diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine (DPPE; tesmilifene) is thought to potentiate the antineoplastic effect of cytotoxic drugs. In a phase III randomized trial for metastatic breast cancer using doxorubicin with or without DPPE, addition of the latter resulted in a significant improvement in overall survival and a trend toward a difference in progression-free survival but, ...