The direct interaction of the antibiotic primycin with the plasma membrane was investigated by employing the well-characterized ergosterol-producing, amphotericin B-sensitive parental Candida albicans strain 33erg+ and its ergosterol-less amphotericin B-resistant plasma membrane mutant erg-2. Th...

With the increasing emergence of antibiotic resistances old antibiotics became a valuable source to find agents suitable to address this problem. More than 20 years after the last report, our purpose was to re-evaluate the in vitro antibacterial activity of the topical agent primycin against cur...

Primycin-sulphate is a highly effective compound against Gram (G) positive bacteria. It has a potentially synergistic effect with vancomycin and statins which makes primycin-sulphate a potentially very effective preparation. Primycin-sulphate is currently used exclusively in topical preparations...

The work presents a synthetic route to the CD ring of calicheamicin and in the case of neocarzinostatin an approach to a functionalised cyclopentane-1,3-diol containing the naturally occurring naphthoate and a glucosamine motif. In the case of the NCS derivative some biological activity (cytotox...

It is assumed that the efficient antitumor activity of calicheamicin γ1 is mediated by its ability to introduce DNA double-strand breaks in cellular DNA. To test this assumption we have compared calicheamicin γ1-mediated cleavage of cellular DNA and purified plasmid DNA. Cleavage of purified p...

The aglycon, or so-called ‘warhead’ portion, of several potent 10-membered ring enediyne antitumor antibiotics contain dienonecarbamate and enediyne chromophores in an unusual bicyclic ring structure in which these two subunits are essentially orthogonal to each other. The circular dichroism (...

Calicheamicin, γ1I, is a remarkable DNA binding-cleaving, enediyne-containing, natural product that exhibits potent antitumor activity. In this study, we used electronic circular dichroism spectroscopy to monitor potential drug-induced DNA conformational changes and DNA induced conformational c...

Treatment of the salt CF3CCLi with alkyl chloroformates affords the compounds CF3CCCO2R (R  Et and CH2Ph) in relatively low yield and with gaseous carbon dioxide yields the acid CF3CCCO2H. Reaction of the acid with diazomethane gives the methyl ester which, with an excess of the reagent,...

A simple and reliable method for the preparation of 2,2-dimethyl-5-(trifluoroacetyl)-1,3-dioxane-4,6-dione and 2,2-dimethyl-6-(trifluoromethyl)-4H-1,3-dioxin-4-one on a multigram scale was developed. These (trifluoroacetyl)ketene precursors were used in the hetero-Diels-Alder reaction with dialk...

IntroductionThis double-blind, randomized controlled trial compared the safety and efficacy of subcutaneous epoetin alfa-epbx, an epoetin alfa biosimilar, with the reference product, epoetin alfa, in hemodialysis patients with end-stage kidney disease and anemia who were receiving epoetin alfa m...

The antitumor platinum(II) compound, [Pt(dach)(Glu)] (dach=trans(±)-1,2-diaminocyclohexane, Glu=glutamate) was formulated with a stealth liposome to improve its biological activity. Liposomes were composed of PC/PEG2000-PE/CH (PC=1,2-diacyl-glycero-3-phosphocholine; PEG2000-PE=poly(ethylene gly...

Multifunctionalized 1,2,3,4-tetrahydropyridines are concisely synthesized in good yields via l-proline-catalyzed or l-proline/FeCl3-cocatalyzed one-pot multicomponent reactions (MCRs). The MCRs involve a domino hydroamination/prins reaction/Mannich-type reaction/intramolecular dehydration–cycli...

Chagas disease (human American trypanosomiasis), which is caused by the protozoan parasite Trypanosoma cruzi, is responsible for numerous deaths each year; however, established treatments for the disease are limited. Differentiation-inducing factor-1 (DIF-1) and DIF-3 are chlorinated alkylphenon...

DIF-1 (differentiation-inducing factor-1; 1-(3,5-dichloro-2,6-dihydroxy-4-methoxyphenyl)hexan-1-one) is a putative morphogen that induces stalk cell formation in the cellular slime mold, Dictyostelium discoideum. It has been previously reported that DIF-1 exhibits anti-tumor activity in mammalia...

2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD; dioxin), a member of a class of environmental pollutants represented by polychlorinated dibenzo-p-dioxins and dibenzofurans, is one of the most toxic artificial compounds ever developed. In this study, we identified a novel TCDD target gene, DIF-3 (diox...

In this study, the structural and vibrational properties of Meldrum’s acid derivative 5-(5-Ethyl-1,3,4-thiadiazol-2-ylamino)methylene-2,2-dimethyl-1,3-dioxane-4,6-dione, C11H13N3O4S were studied combining experimental techniques such as Raman and FT-IR spectroscopy and density functional theory...

Chiral 1H-pyrazolo[3,4-b]pyridines fused with nopinane frame were obtained by FeCl3-catalyzed assembling of pinocarvone oxime and 1-aryl-1H-pyrazol-5-amines. Chemical structures of new compounds were solved by NMR spectroscopy and confirmed by quantum chemical calculations and X-ray crystallography.

Cyclo(-Phe(p-NH[1-14C]Ac)-Trp-Lys-(CO(p-N3)C6H4)-Trp-Phe-dPro), in the following named azidobenzamido-008, was synthesized in order to identify binding sites for c(Phe-Thr-Lys-Trp-Phe-dPro), named 008, (a cyclosomatostatin with retro sequence) in liver cell plasma membranes. In the dark the abov...

A convenient synthesis of three new amino acids, L-α-(3-phenylpropyl)-glycine, L-α-(2-benzyl-3-phenylpropyl)-glycine and its conformationally constrained analog, trans-4-benzyl-cis-5-phenyl-L-proline is reported. All compounds were prepared in good diastereomeric or enantiomeric purity from L-...

Mesylates or tosylates of δ-hydroxy-l-norvaline esters spontaneously afford l-proline esters upon exposure to aqueous buffer in near quantitative yield. This novel reaction has led to the development of a simple route to optically active proline esters.