Showing papers in "Bioorganic Chemistry in 2010"

TL;DR: A series of new alpha,beta-unsaturated conjugated ketones containing ferrocenyl pyrazole unit were synthesized and fully characterized by IR and NMR spectroscopy and exhibited a better cytotoxic activity in the cell growth inhibition of K562 cell lines in comparison with cisplatin as a reference compound.

TL;DR: It was found that juglone acted as a strong, time and concentration dependent inactivator of urease and lawsone showed an inconsiderable inhibition influence, while lawsone well reacted with l-cysteine, poorly with glutathione and hardly with Urease thiols.

TL;DR: The calculation results reveal that the driving forces for ring-closing reactions in the two different systems are proximity orientation of the nucleophile to the electrophile and the ground strain energies of the products and the reactants.

TL;DR: Peptides containing L-N(epsilon)-acetyl-lysine (L-AcK) or its side chain modified analogs were prepared and assayed using SIRT1, the prototypical human silent information regulator 2 (Sir2) enzyme, and showed that SIRT 1 catalyzed the stereospecific deacetylation of L- AcK versus its D-isomer.

TL;DR: The low synthetic cost, green synthetic protocols, easy one-step synthesis from commercially available and cheap reagents as well as the very good antileishmanial activity obtained for 14 and 16 indicates that these MBHA can be a novel and promising class of anti-parasitic compounds.

TL;DR: Observations suggest that the structurally-simplified analogs to rosmarinic acid, compounds 1 and 3, might be the base of therapeutic strategies to prevent thrombotic complications associated to platelet hyperaggregability due to oxidative stress.

TL;DR: In search of an activity-preserving protein thiophosphorylation method, potassium thiPhosphoramidate and diammonium thiophile salts in Tris- and ammonium carbonate based buffer solutions were employed, proving to serve as a non-destructive environment.

TL;DR: A new class of inhibitors of herpes simplex virus replication was found derived from condensed 1,2,4-triazolo[5,1-c][1, 2,4]triazines and 1,1,5-a]pyrimidines, structural analogues of natural nucleic bases, which could be a key enzyme of viral replication.

TL;DR: For constructing a bifunctional antioxidative enzyme with both superoxide dismutase (SOD) and glutathione peroxidase (GPx) activities, a supramolecular artificial enzyme was successfully constructed by the self-assembly of the Mn(III)meso-tetra[1-(1-adamantyl methyl ketone)-4-pyridyl] porphyrin and cyclodextrin-based telluronic acid through host

TL;DR: Allocolchicinoids with B- and C-ring variations were synthesized using sequential enyne-metathesis/ Diels-Alder reactions and evaluated for their inhibitory effect on tubulin assembly in vitro.

TL;DR: In this article, the Morita-Baylis-Hillman adduct (MBHA) 3-hydroxy-2-methylene-3-(4-nitrophenyl)-propanenitrile (3) was synthesized and evaluated on Trypanosoma cruzi epimastigote and bloodstream trypomastigot forms.

TL;DR: The optimized expression, isolation, and purification of HpAgD, and the development and characterization of a novel class of haloacetamidine-based Hp AgD inactivators, which are the most potent AgD inhibitors ever described are described.

TL;DR: Synthesis of stilbene-fused chalcones and flavanones were successfully completed and molecules were designed in a way to mimic the structural features of both "stilbenes and chalCones" or "stILbene and Flavanones" at the same time, and synthesized by three steps.

TL;DR: Human TS exhibits unaltered K(m) values for dUMP and N(5,10)-methylenetetrahydrofolate, but a 50% lower turnover number, pointing to a strong influence of Ser(124) phosphorylation on its catalytic efficiency.

TL;DR: Ring contraction of 2,5-diketopiperazines by TRAL-alkylation led to the stereoselective synthesis of original pyrrolidine-2,4-diones, a novel series of promising molecules with moderate anti-proliferative activity on breast cancer cells.

TL;DR: It is shown that cleavage also proceeds through a pH-independent mechanism, and rate constants were determined as a function of temperature at pH 7 and a linear Arrhenius plot was constructed.

TL;DR: The thermal stability of the fully phosphorothioated ASOs was obtained by only replacing 20% of the oxygen of the phosphodiester moiety, indicating that the antisense sequences need not to be PS backbone.

TL;DR: A protection-selective deprotection sequence followed by oxidation of the free hydroxyl group at the 2'-position of the dideoxy benzoylated analogues with simultaneous elimination reaction of the beta-benzoyl group gave the desired nucleosides 6c-e.

TL;DR: The association constants of differently protonated forms of kanamycin A with sulfate and enthalpy changes for protonation of each amino group were determined and it was observed that changes in chemical shifts of all atoms in ring C were controlled by ionization of a single amino group with pK(a) 7.98; this resolves the previously existed uncertainty in assignment of protonations sites in rings B and C.

TL;DR: This work explored the ability of PNA and PNAs with modified monomers to bind to DNA and to interfere in the formation of DNA/transcription factor complex.

TL;DR: It was demonstrated that the gene product of cinD exhibits (1R)-6beta-hydroxycineole dehydrogenase activity, the second step in the degradation of 1,8- cineole.

TL;DR: It was shown, that cultured ex vivo human T-Lymphoblastoid (CEM) cells respond to synthesized thiocolchicine and fluorine thiocolateine derivatives, and the results of the multi-technique approach are consistent with the fact that the new derivatives are more efficient than colchicines and thi Chocolateine ex vivo.

TL;DR: Michael addition reactions of ethanethiol with 6-bicycloaryl substituted 5,6-dihydro-2H-pyran-2-ones were studied and revealed that biological activity depends on the existence of a Michael acceptor, but potency probably depends upon the 3D structure of the substituent on lactone ring.

TL;DR: This study showed that at pH<3.0 the Au( III) ion was able to deprotonate the amide nitrogen atom, however this displacement reaction was very slow and the total concentration of the corresponding Au(III)-peptide complex formed after 5 days was less than 60% for the Gly-L-Ala or 70% forThe Gly-Gly dipeptides.

TL;DR: The preparation of 1-deoxy-d-xylulose 5-phosphate, the key intermediate of MEP biosynthetic pathway for terpenoids by using recombinant 1- deoxy- d-xymethine 5- phosphate synthase of Rhodobacter capsulatus was optimized.

TL;DR: It was concluded that the specificity determining factors which govern substrate recognition by the enzyme should be grouped along the phosphorylatable substrate, and such clustering might open new perspectives for pharmacophore design of peptides and peptide-like ligands.

TL;DR: The nucleus-independent chemical shift (NICS) indices of aromaticity, calculated for four boron compounds, 4-hydroxy-5,6-dihydroborauracil, 4.hydroxyborauricil, and parent uracil were analyzed in parallel with the NMR properties, in order to learn more about the aromaticity of those heterocyclic systems.

TL;DR: The diamino derivatives 5 and 6, which are active against influenza A H3N2 virus although less potent than amantadine and its equipotent spiropiperidine 4, are identified.

TL;DR: A new class of enolphosphates derivatives, the 1-alkenyldiphosphates, showed interesting in vitro antibacterial activities against Gram-positive bacteria and Gram-negative pathogens including Pseudomonas aeruginosa and Escherichia coli.

TL;DR: It can be concluded that glycine caps are useful, as they reduce helical unravelling and enhance helicity, and thus, glycine will be included as a C-terminal residue in future de novo peptide sequences.