Showing papers in "Bioorganic & Medicinal Chemistry in 1995"

TL;DR: Comparative fluorescence and hydrodynamic studies using the proven intercalator ethidium and the groove binder Hoechst 33258 demonstrate reliable criteria that may be used to distinguish intercalation from groove binding in the absence of high resolution structural data.

TL;DR: Flexible molecules change their conformation upon binding to a protein different from that in the crystal structure and also from that of the global energy minimum, and the degree of deformation depends upon the number of freely rotatable bonds in the molecule.

TL;DR: Antimicrobial activity of a series of long-chain alcohols and common naturally occurring alcohols were tested against 15 selected microorganisms in order to gain new insights into their structural functions.

TL;DR: Activity in this assay did not correlate well with inhibition of thrombin-induced cleavage of a synthetic substrate, presumably a consequence of inherent chemical instability and degradation in plasma.

TL;DR: As judged by their ability to inhibit stimulated LTB4 biosynthesis in human neutrophils, compounds 1a-1d all turned out to be highly potent 5-lipoxygenase inhibitors with IC50-values ranging from 0.40 microM for 2-benzyl-1-naphthol (1a) to 0.063 microM as judged by cyclic voltammetry.

TL;DR: This review covers the recent advances in the development of highly potent inhibitors of platelet aggregation as potential therapeutic drugs for thrombosis related to cardiovascular and cerebrovascular diseases.

TL;DR: Development of small molecule thrombin active site inhibitors has been an area of intense research and a brief review on recent progress and challenges is outlined.

TL;DR: 3'-End-modified oligomers were significantly stabilized towards 3'-exonucleolytic degradation compared to unmodified analogues and showed acceptable hybridization properties as measured by UV experiments.

TL;DR: It is concluded that transnitrosation or enzymatic cleavage are obligatory steps in the mechanism of NO release from GSNO, whereas SNAP needs only the presence of metal ions to effect this process.

TL;DR: An extensive study of analogs of the potent antitumor antibiotics CC-1065 and the duocarmycins which incorporate the 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) alkylation subunit proved to be potent cytotoxic agents and efficacious antitumors compounds.

TL;DR: Doxorubicin was modified with five different heterobifunctional reagents to produce drug analogs containing 3'-N-amide or C-13 hydrazone linkage with maleimide, which are not active in vitro, however, Dox(hydrazone-linked) immunoconjugates are selectively toxic to the CEA positive cell line.

TL;DR: It is proposed that anthracene-9-carbonyl-N1-spermine intercalates in at least two different binding orientations with poly(dAdT)2, and it is deduced that the ligand can intercalate from both the minor groove and the major groove.

TL;DR: The observed formation of potentially toxic 6-nitrocatecholamines under physiologically relevant conditions may open new perspectives to an understanding of the biochemical processes underlying NO-induced toxicity and neuronal degeneration.

TL;DR: In order to improve the available methods to produce an immunoconjugate the use of longer heterobifunctional cross-linking reagents were investigated and two new maleimidobenzoyl spacers have been synthesized in a one step process from 4-maleimidOBenzoic acid.

TL;DR: A glycopeptide carrying a pentasaccharide core structure of asparagine-linked glycoproteins was synthesized and coupled with an aspartic acid derivative to furnish an Asn-linked oligosaccharides in a protected form.

TL;DR: Three new thrombin and trypsin inhibitors, cyclotheonamides C, D, and E, were isolated from the marine sponge Theonella swinhoei by spectral and chemical methods.

TL;DR: The result indicates that RES-701-1 adopts an extraordinary folding; the 'tail' (Trp10-Trp16) passes through the 'ring' region (Gly1-Asp9) and several critical NOEs directly support this extraordinary folding.

TL;DR: The 4-substituted phenyl phosphorodiamidates (4-R-PhOP(=O)(NH2)2) are slow-binding inhibitors of H. pylori urease with no evidence of kinetic saturation, suggesting that Urease inhibition is covalent but reversible, involving a common phosphoacyl enzyme intermediate.

TL;DR: The dimeric dye ethidium homodimer is found to bis-intercalate in the triplex as well as the duplex but, in contrast to the monomers, no variation in geometry between duplex and triplex is observed.

TL;DR: Both syntheses were carried out in four enzymatic steps and one or two chemical deprotection steps routinely used in peptide synthesis, and the overall yields of pentapeptide derivatives were between 40-54% of pure product.

TL;DR: A series of isoxazoline derivatives were synthesized and investigated for their in vitro inhibitory activity towards human leukocyte elastase, cathepsin G and proteinase 3.

TL;DR: Three DHAP-dependent aldolases have been cloned and overexpressed in Escherichia coli using two different expression vectors and the effects of cultivation temperature and concentration of inducer have been studied in order to optimize the expression of the recombinant proteins and to avoid the formation of inclusion bodies.

TL;DR: Results indicate that the Watson-Crick hybridization of PNAs to duplex DNA by strand displacement is favored by the presence of potential alternative secondary structures within the target sequence.

TL;DR: The antitumor activities of some Fe(II)/Fe(III) complexes containing 1,3-diacetyl-2H-benzimidazole-2-thione along with a few derivatives of 1,2,4-triazol, 1,1,3, 4-oxadiazole and 1,5,5-thiadiazoles as co-ligands have been investigated.

TL;DR: The design and synthesis of a number of potent beta-amino hydroxylamine and amino hydroxamic acid inhibitors of leukotriene A4 hydrolase are described and it was found that having a free amine was essential for high activity.

TL;DR: 4-Benzylaminoquinazolines can be potent reversible inhibitors of the EGFR tyrosine kinase at the ATP binding site, and it is suggested that the best of these inhibitors can induce a conformation of the kinase not available to poorer inhibitors.

TL;DR: Six novel docetaxel analogues that possess a N-(7-nitrobenz-2-oxa-1,3-diazo-4-yl)amido-6-caproyl chain in position 7 or 3' have been synthesized, demonstrating that the microtubule cytoskeleton constitutes their main subcellular localization.

TL;DR: Several iron complexes in combination with hydrogen peroxide (HOOH) catalytically hydroxylate aromatic substrates (ArH) and other substituted benzenes (PhX) undergo addition by free HO at the ortho and para aryl carbons to give Ar-Ar as the predominant product.