Showing papers in "Bioorganic & Medicinal Chemistry in 2001"

TL;DR: A pivotal path forward would be to understand in a predictive mechanistic sense how to create ensembles of weak bonds between synthetic ligands and biological macromolecules in water, the solvent of life.

TL;DR: The in vitro selection of nucleic acid binding species (aptamers) is frequently repetitive, time-consuming, and poorly adapted to high-throughput applications as discussed by the authors ; however, the increases in throughput brought about by automation should potentiate the application of aptamer technology to the rapidly growing field of proteomics.

TL;DR: The purpose of this account is to foster a synergy between the two expanding research areas of glycomimetics and glycosyltransferases.

TL;DR: The synthesis, in vitro antifungal evaluation and SAR study of 41 chalcones and analogues and all active structures tested for their capacity of inhibiting Saccharomyces cerevisiae beta(1,3)-glucan synthase and chitin synthase, enzymes that catalyze the synthesis of the major polymers of the fungal cell wall.

TL;DR: Novel sulfonamide inhibitors of the zinc enzyme carbonic anhydrase prepared by reaction of aromatic or heterocyclic sulfonamides containing amino, imino, or hydrazino moieties with N,N-dialkyldithiocarbamates showed potent inhibition of growth against several leukemia, non-small cell lung, ovarian, melanoma, colon, CNS, renal, prostate and breast cancer cell lines.

TL;DR: The success of both in vitro and in vivo synthesis of taxadiene bodes well for the future production of taxoids by non-paclitaxel producing organisms through pathway engineering.

TL;DR: The mode of binding of tetracycline to the cb28 aptamer resembles its interaction with the primary binding site on the small ribosomal subunit.

TL;DR: In this paper, a plausible new prebiotic synthesis of naturally occurring purine and pyrimidine derivatives from formamide under catalytic conditions was reported, and the role of catalysts showed to be not limited to the improvement of the yield but also relevant in providing a high selectivity in the products distribution.

TL;DR: Seven new withanolide glycosides called withanosides I, II, III, IV, V, VI, and VII were isolated from an Indian natural medicine, Ashwagandha, the roots of Indian Withania somnifera DUNAL.

TL;DR: The methanolic extracts from five kinds of rhubarb were found to show scavenging activity for DPPH radical and .O2- and several stilbenes with both the 3-hydroxyl and 4'-methoxyl groups inhibited xanthine oxidase.

TL;DR: Out of the twelve chalcones tested, three were found to exhibit potent anti-invasive activity and a prenylated acetophenone carrying two methoxy groups and two free phenolic hydroxy functions was found to be a potential antioxidant.

TL;DR: In this paper, the authors reported that 2′-O,4′-C-methylene bridged nucleic acid (2′, 4′-BNA) modification of triplex-forming oligonucleotide (TFO) significantly enhances the binding affinity towards target dsDNA.

TL;DR: This review discusses what is known about apoptotic pathways and its implication for normal cellular function and describes the characteristic morphological changes of apoptosis.

TL;DR: Some simple isoquinoline alkaloids were significantly active in each assay, and may be useful as lead compounds for developing potential chemotherapeutic agents.

TL;DR: Novel indolylpyrimidines and indolylpyrazines have been synthesized as potential antitumor agents and displayed selective cytotoxic activity against IGROV1 tumor cell line with the GI(50) value below 0.01 microM.

TL;DR: Quantification of CLB2 expression at the RNA and protein levels by RT-PCR and Western blot analysis demonstrates that the aptamer ligand regulates transcript translatability rather than stability, consistent with a model in which translational initiation is blocked by ligand-induced conformational changes in the 5'-UTR.

TL;DR: A series of N-substituted N-nitrosohydroxylamines including six new compounds were synthesized and examined for inhibition of mushroom tyrosinase, showing the most potent activity, as powerful as that of tropolone, one of the most powerful inhibitors.

TL;DR: Structural-immunostimulatory activity relationships of phosphorothioate oligodeoxynucleotides containing YpG- and CpR-motifs containing Y and R stand for pyrimidine and purine analogues are examined to understand the critical role of each functional group of the cytosine and guanine moieties in a CpG -motif in inducing immunostimulation activity.

TL;DR: It has been possible to map specific regions of the human hemoglobin molecule that are responsible for significant antimicrobial activity and it is conceivable that, in addition to its role in oxygen transport, hemoglobin functions as an important multi-defense agent against a wide range of microorganisms.

TL;DR: The synthesis and anti-inflammatory activity of 4,5-dihydroxy-3-methyl-1H-pyrazolo[3,4-c]pyridazine-4, 5-diamine and 3- methyl-N4,N5-bis[4-benzimidazol-2yl](4-methylphenyl]-1H

TL;DR: The hypoxia-selective DNA-cleaving properties of 4 reported here may provide a chemical basis for understanding the cytotoxic and mutagenic activities of various quinoxaline 1,4-dioxide antibiotics.

TL;DR: The structure-activity relationship of the chemical series was conducted and several analogues displaying sub-nanomolar K(i) values at the EP3 receptor and micromolar activities at theEP1, EP2 and EP4 receptors were found.

TL;DR: A copper-dependent self-cleaving DNA that was isolated by in vitro selection has been minimized to its smallest active domain using both in vitroselection and rational design methods.

TL;DR: In this article, a carbamoyl phenyl ring substituted at 3 and 4 position with NO 2 group or 2 position with Cl or OCH 3 group showed >90% inhibition against H 37 Rν comparable to other substituted phenyls.

TL;DR: Five new constituents including a flavonoid, artemisidin A, and four coumarins, artemicapins A, B, C, C and D, together with 70 known compounds, have been isolated and characterized from the aerial part of Artemisia capillaris.

TL;DR: SELEX (Systematic Evolution of Ligands by EXponential enrichment), a combinatorial method that employs biopolymers for drug discovery, was applied to identify single stranded DNA sequences able to bind L-Tyrosinamide, a simple mimic of Tyrosine, an amino acid essential to the catalytic activity of several enzymes of pharmaceutical interest.

TL;DR: A new class of N,N-diethyl-(2-arylpyrazolo[1,5-a]pyrimidin-3-yl)acetamides (3f-y), as azaisosters of Alpidem, was prepared following a novel synthetic method and their affinities for both the peripheral (PBR) and the central (CBR) benzodiazepine receptors were evaluated.

TL;DR: Results can be explained by the different reactivity and equilibrium conditions for thiol addition of the two reactive centers of bifunctional STLs in cellular test systems and verified a clear correlation between the different reactsivity of their electrophilic centers and the observed biological effects in in-vitro cell systems.

TL;DR: 4-Trifluoromethyl-2,6-bis[3'-(N-tosyl-6'-methoxylindolyl)]pyridine 18 was identified as the most potent in this series and evaluated for cytotoxic activity against P388 and A-549 cells with IC(50) values.

TL;DR: It is found that further modulation and improvement in potency at inhibiting HMG-CoA reductase was obtained by having the optimal substituents flanking the desmethylmevalonic acid portion, that is, 4-fluorophenyl and cyclopropyl, instead of the usual isopropy group.