An international journal for the quickest publication of high-quality research covering the breadth of synthetic, physical and biomolecular organic chemistry.
OBC cover gallery 2007
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Cover Gallery
Pyrazole carboxamides and carboxylic acids as protein kinase inhibitors in aberrant eukaryotic signal transduction: induction of growth arrest in MCF-7 cancer cells.
DOI: 10.1039/B711279C
Effects of b-substituents (R) on the redox behaviour of cyclic nitroxyl radicals, used as spin probes as well as antioxidants, have been investigated by using electrochemical techniques. The electron-donating substituents caused negative shift in the one-electron oxidation and reduction potentials of the nitroxyl radicals, while the substituents with electron-withdrawing effect behaved reversely.
DOI: 10.1039/b717659g
An indole quinone-camptothecin conjugate (IQ-CPT) prodrug targets tumor-specific hypoxic microenvironments, and is activated via one-electron reduction by intracellular reducing enzymes or an external trigger such as ionizing radiation. This releases free camptothecin (CPT), which is a potent inhibitor of DNA topoisomerase, inducing irreversible and lethal strand breaks in DNA.
DOI: 10.1039/b716857h
A swallow-tailed perylene derivative including a triphenylphosphine moiety was synthesized and applied to the selective fluorescent imaging of lipid hydroperoxides in cell membranes using visible light.
DOI: 10.1039/b716858f
The design, synthesis and applications of alpha-helices and mimetics, in the last 5 years including non-peptidic scaffolds, modified peptide backbones that mimic the recognition properties of alpha-helices, miniature proteins and synthetic foldamers have delivered promising lead compounds for biological applications.
DOI: 10.1039/b710425a
Three families of synthetic helical bundle proteins containing different peptide sequences within the bundles are described. These first generation hetero-TASPs represent prototypes for potentially more sophisticated de novo proteins.
DOI: 10.1039/b716081j
A young male Heliconius pachinus approaching an already mated female carrying the macrolides. The female exposes its abdomial scent glands to repel the male.
DOI: 10.1039/b710284d
Atomic force microscopy is used to monitor the force-induced unfolding of a protein along a predefined reaction coordinate. The force required to unfold a protein represents the protein's mechanical stability, which can be tuned using protein engineering techniques.
DOI: 10.1039/b715246a
The cover image shows strategies for the generation of natural product derivatives, exemplifying pathways leading to the epothilone derivative ZK-EPO (total synthesis), the ansamitocin derivative DM1 (semisynthesis) and various avermectin derivatives (mutasynthesis), while indicating steps requiring microbial producers such as actinomycetes.
DOI: 10.1039/b709549j
Cascades involving nitrogen-directed homoallylic radical rearrangements lead to a variety of bioactive azacycles
DOI: 10.1039/b707566a
Superimposed images of the bismuth(III)-catalysed Mannich-type reaction onto a bismuth crystal taking the exact shape of the Mayan pyramid of Kukulkan in Chichen Itza (Mexico). A wide variety of ?-amino ketones and ?-amino esters can be accessed very efficiently with high yields.
DOI: 10.1039/b713670f
The intramolecular cation-pi interaction is effective as a conformation-controlling tool. The blocking of the pyridinium face allows a face-selective reaction to give stereo-controlled products.
DOI: 10.1039/b706512b
Dual aromatase-sulfatase inhibitors represent a novel strategy in oncology drug discovery. The cover shows the novel dual inhibitor (compound 11), docked into the superposed aromatase (yellow) and steroid sulfatase (magenta) enzymes, adopting different conformations to bind to and inhibit the dissimilar active sites of either enzyme.
DOI: 10.1039/b712587a
N-Substitution of aminoterpyridines was found to be a simple and useful way to tune both the radiation energy and solvent susceptivity of their fluorescence.
DOI: 10.1039/b707662b
The cover image shows a simple SNP typing method by using sequence specific interstrand photocrosslinking via p-carbamoylvinyl phenol nucleosides.
DOI: 10.1039/b708264a
The cover picture displays the genesis of molecular electronics with the first hypothesised single-molecule rectifier in the centre and the chronological development of the area in the timeline at the bottom. The central molecule combines electronic functionality on the left with molecular design on the right. The complexity of the interface between molecular reality and the macroscopic world is reflected by the yellow and grey shadows and silhouettes in the back.
DOI: 10.1039/b703287k
The ability of chemically synthesized artificial proteins to bind metal ions was demonstrated by inductively coupled plasma mass spectrometry (ICP-MS) and other biophysical techniques.
DOI: 10.1039/b704159d
Several distinct chiral poly rare earth metal complexes can be generated from structurally resembling chiral ligands, depending on the assembly states of the structural modules. These "assemblymers" produced completely distinct functions as asymmetric catalysts. This characteristic of the poly rare earth asymmetric catalysts mimic natural functional molecules, proteins.
DOI: 10.1039/b704542e
Bacterial adherence fibers, pili, are crucial for the initiation and advancement of urinary tract disease. Pilicides (2-pyridones) have been shown to interfere with periplasmic chaperones and thereby block assembly of pili. Electron micrographs courtesy of Jana Jass.
DOI: 10.1039/b702397a
The image shows the generic molecular rotor structure in the center (as shown in the graphical abstract) with the green background hinting at its fluorescence emission color. Four applications are shown, clockwise starting top left: Laser-induced fluorescence emission under Couette shear, cell cytoplasm stained with a hydrophilic molecular rotor, emission and excitation spectra in fluids of different viscosity, and fluorescence emission in a flow chamber.
DOI: 10.1039/b618415d
The picture illustrates an interaction between human antibody 2G12 and a synthetic template-assembled oligomannose cluster. The synthetic neoglycopeptide immunogen was designed as a candidate HIV-1 vaccine.
DOI: 10.1039/B702961F
The structural properties of DNA block copolymer micelles can be switched from spherical objects into rod-like aggregates by hybridization. Moreover, these bioorganic hybrid materials find increasing importance in the fields of biotechnology, nanoscience and biomedicine.
DOI: 10.1039/B617941J
Stable radicals have long fascinated chemists and are finding uses in a wide selection of applications. This perspective highlights developments in stable radical chemistry, focusing on fundamental aspects of radical stability.
DOI: 10.1039/b705511k
The Medusa relief sculpture (from the theatre in Perge, Turkey, 2nd Century A.D.) shows in the four corners opium poppy capsules (seed pods after blooming from which opium is obtained) on the stalk. The oval objects in the inner diamond surrounding the man's face are the unopened bloom pods of the opium poppy. The expression on the man's face may have been meant to express both the good (medicinal value) and the bad (addictive) effects of opium.
DOI: 10.1039/b618875c
A lipid-membrane-incorporated C60 induced cell death under visible light irradiation. In the picture, a liposome is compared to a "Mari", which is a "Japanese traditional hand-made ball" coated by colourful threads.
DOI: 10.1039/b704332p
A concise stereoselective synthesis of orthogonally protected lanthionine and beta-methyllanthionine. The image was designed by Annie Tykwinski.
DOI: 10.1039/b618178c
Carbohydrate post-glycosylational modifications (PGMs) are modifications taking place on the carbohydrate structures after the formation of the glycosidic bonds. Studies in this emerging area include identifying carbohydrates with PGMs, finding and characterizing proteins that catalyze the formation of PGMs, developing methods for synthesizing carbohydrates with PGMs, and establishing assays to elucidate the importance of carbohydrate PGMs.
DOI: 10.1039/b700034k
Superimposed pictures of palytoxin dimer (left) and palythoa tuberculosa (right) onto a X-ray scattering image of palytoxin in aqueous solution.
DOI: 10.1039/b702774p
Singlet oxygen may be used to elegantly synthesise the bis-spiroketal motif of salinomycin, a natural product harvested from a Streptomyces broth.
DOI: 10.1039/b617966e
The picture illustrates a delphi surface representation of the interface between VIF and ElonginB-ElonginC. The interface was considered to be a novel target for anti-HIV drug design.
DOI: 10.1039/B612050D
Complexation with cobalt(III) has been used to assemble the kinetically robust [3]rotaxane shown here.
DOI: 10.1039/B616621K
Self-assembled nanostructures, excellent platforms for displaying multiple carbohydrate ligands, have vast potentials to be utilized in modulating carbohydrate-dependent biological multivalent interactions.
DOI: 10.1039/b700402h
Pyrrolidine amide oliogonucleotide mimics (POM): Potential solutions from zebrafish developmental biology through to high throughput DNA sequencing.
DOI: 10.1039/B613384N
Developing the right catalyst for a desired reaction is not an easy task: preparing libraries of ligands increases the changes of success.
DOI: 10.1039/b618223m
Polymer chain growth from a protein macroinitiator results in the protein-polymer conjugate. Image created by Mike Britton. Protein structure from the Protein Data Bank, PDB ID: 1P56, M. Sagermann, W. A. Baase, B. H. M. Mooers, L. Gay, B. W. Matthews, Biochemistry, 2004, 43,1296-1301
DOI: 10.1039/B612355D
The cover image shows the nonenzymatic terminal labeling of oligoribonucleotide by using template-directed photoligation through 5-carboxyvinyl-2´-deoxyuridine
DOI: 10.1039/b617472h
