Showing papers in "Bioorganic & Medicinal Chemistry in 2005"

TL;DR: Recent advances in tumor-targeting drug conjugates including monoclonal antibodies, polyunsaturated fatty acids, folic acid, hyaluronic acid, and oligopeptides are described as tumor- targeting moieties.

TL;DR: Compounds 1, 3, 12, and 14-16 can serve as new leads for further development of anti-AIDS agents as well as other benzylisoquinoline, aporphine, and bisbenzylisoquoline alkaloids, which were previously isolated from the leaves and embryo of Nelumbo nucifera and evaluated for anti-HIV activity.

TL;DR: It is found that all anthocyanidin glycosides were hydrolysed by the microflora within 20 min and 2 h of incubation depending on the sugar moiety, and phenolic degradation products were already detected after 20 min of incubations.

TL;DR: Four important anticancer leads are focused on, that is, camptothecin, taxol, combretastatin A-4 and podophyllotoxin, whose chemistry, structure and activity relationships, biological activities, modes of action, analogue synthesis and future prospects have been discussed.

TL;DR: The results of spectroscopic measurements and the thermodynamic parameters obtained suggest that hydrophobic interaction is the predominant intermolecular forces stabilizing the complex, which is also good agreement with the results of molecule modeling study.

TL;DR: Oligomeric mini-proteins, short peptides with discrete protein-like structures, may serve as valuable models for understanding features of protein oligomerization.

TL;DR: A group of mono-, di-, tri- and tetra-substituted hydroxychalcones are introduced as effective tyrosinase inhibitors, showing that the most important factor determining tyros inase inhibition efficiency is the position of the hydroxyl group(s) rather their number.

TL;DR: The natural product curcumin, obtained from the spice turmeric, exhibits numerous biological activities including anti-cancer, anti-inflammatory, and anti-angiogenesis activities; some of these biological activities may derive from its anti-oxidant properties.

TL;DR: The review discusses the significance of mucin-type O-linked glycosylation initiated by the polypeptide N-acetylgalactosaminyltransferases in biology and development of chemical tools to study these enzymes and their substrates.

TL;DR: Chelator 9 (HLA20), having good permeability into K562 cells and moderate selective MAO-B inhibitory activity (IC50 110 microM), displayed the hightest protective effects against differentiated P19 cell death induced by 6-hydroxydopamine.

TL;DR: Low molecular weight chitosan had stronger scavenging effect on O(2)(.-) and (-.)OH than high molecular weight ChITosan and sulfated chitOSan derivatives and CTS4 showed more considerable ferrous ion-chelating potency than others.

TL;DR: Five derivatives of 5-arylidene-2-imino-4-thiazolidinones exhibited significant activity levels in models of acute inflammation such as carrageenan-induced paw and pleurisy edema in rats, and the ability of such a new class of anti-inflammatory agents to inhibit COX isoforms was assessed in murine monocyte/macrophage J774 cell line assay.

TL;DR: Comparing the photodynamic effect of a cationic Zn(II) N-methylpyridyloxyphthalocyanine and a noncharged ZnPc 1 has been compared in both homogeneous media bearing photooxidizable substrates and in vitro using a typical Gram-negative bacterium Escherichia coli to show that cationIC ZNPc 2 is an efficient phototherapeutic agent with potential applications in photodynamic inactivation of bacteria.

TL;DR: Three new highly selective CB(2) receptor agonists were identified and docking studies indicated that the CB(1) receptor affinities of these compounds were consistent with their aromatic stacking interactions in the aromatic microdomain of theCB( 1) receptor.

TL;DR: The studied results by FT-IR and CD experiment indicated that the secondary structures of protein have been perturbed by the interaction of wogonin with BSA.

TL;DR: Two series of 2-substituted and three new diacetyl benzofurans synthesized through palladium-catalyzed reactions demonstrated mild to significant growth inhibition against antibiotic-susceptible standard and clinically isolated strains of Gram-positive and Gram-negative bacteria as well as human fungal pathogens.

TL;DR: These in vitro results suggested the possibility that sulfated chitosans could be effectively employed as ingredient in health or functional food, to alleviate oxidative stress, and extensive studies need to be conducted to ascertain the in vivo safety of sulfations in experimental animal models.

TL;DR: It was proved that the fluorescence quenching of HSA by CS is a result of the formation of a CS-HSA complex and synchronous fluorescence spectroscopy data and UV-vis absorbance spectra have suggested that the association between CS and HSA changed the molecular conformation of H SA and the electrostatic interactions play a major role in CS-hSA association.

TL;DR: Targeted PDT offers the opportunity of enhancing photodynamic efficiency by directly targeting diseased cells and tissues by delivering photoactive compounds to KB nasopharyngeal cell line, which is one of the numerous tumor cell types that overexpress folate receptors.

TL;DR: It could be concluded that for a better inhibition of tyrosinase, electronegative substitution is essential as most probably the active site of the enzyme contain some hydrophobic site and position is also very important for the inhibition purposes due to the conformational space.

TL;DR: While all simple acetamides are essentially inactive, aromatic amides and amidines have potent antibacterial activities, and aromatic amidine derivatives 13 f-h exhibited the best inhibitory activity against MRSA and MRSE.

TL;DR: Semiempirical AM1 calculations showed that negative electrostatic potentials around oxygen of the phenoxy and nitrogen of the imidazole moieties have direct effect on the antibacterial activity towards S. aureus A 15091.

TL;DR: The induction of biosynthesis of four new diterpenoids was observed following the addition of a marine alpha-proteobacterium to an established culture of the marine-derived fungus Libertella sp.

TL;DR: The approach to the design of adaptable β-peptide scaffolds with high levels of 14-helix structure in water is described and the potential of this strategy for targeting other therapeutically important proteins is examined.

TL;DR: An attempt in correlating the derived physicochemical properties with the HIV-RT inhibitory activity resulted in some statistically significant QSAR models with good predictive ability.

TL;DR: Findings provide a relevant basis for the development of xanthones as an agent for cancer prevention and combination therapy with anti-cancer drugs.

TL;DR: It is heartening to note that the global and local electrophilicity values together can explain the toxicity of a large variety of aliphatic compounds nicely without resorting to any other descriptor or other microscopic/macroscopic physicochemical properties as is the situation in all other QSAR studies.

TL;DR: The curcumin bioconjugates synthesised and characterised by spectra UV, (1)H NMR and elemental analysis are more effective than Cefepime, an antibacterial drug available in market, at the same concentration.

TL;DR: A molecular modelling study was performed to explore the ability of this inhibitor to bind simultaneously to both sites of the enzyme and make it a promising lead for developing disease-modifying drugs for the future treatment of Alzheimer's disease.

TL;DR: A new class of 4-aminoquinoline derivatives based on the natural product isatin scaffold were designed and synthesized for biological evaluation against three strains of the malaria parasite Plasmodium falciparum, and two of the compounds based on a flexible alkyl chain linker and a thiosemicarbazone moiety warrant further investigation as potential anti-plasmodial leads.