Medicinal Chemistry - Volume 3, Issue 5, 2007

During carcinogenesis aberrant N-glycosylation may lead to the development of subpopulations of tumor cells with altered adhesion properties and increased invasive potential. Biosynthesis of glycans and oligosaccharides is tissue- specific and developmentally regulated by number of glycosyltransferases of which fucosyl-, sialyl- and Nacetylglucosaminyltransferases often participate in synthesis of tumor type glycans. Read More

In the search for effective, selective, and nontoxic antiviral and antitumor agents, a variety of strategies have been devised to design nucleoside analogues. Here we have described the versatile synthesis of β-L-1,3- thiazolidine nucleoside analogues. These analogues are all derived from the key stereochemically defined intermediate Ntert- butoxy-carbonyl-4-hydroxymethyl-1,3-thiazolidine-2-ol which was accessible in 57% yie Read More

The synthesis of a series of 6-aryl-4-oxohexanoic acids is described: This involves condensation of an appropriate aldehyde (Ia-f) and levulenic acid using catalytic amounts of piperidine and acetic acid in toluene to afford the 6- aryl-4-oxohex-5-enoic acids (IIa-f).The arylidene derivatives (IIa-d) were reduced by hydrogen at room temperature using palladium (10 %/carbon) as catalyst to produce 6-aryl-4-oxohexanoic acids (IIIa- Read More

Taking into account that compounds bearing a thiazolyl, pyridyl and indolyl, moieties possess a wide spectrum of biological activities which is related to their capacity to transfer electrons and to scavenge reactive oxygen species (ROS), we synthesized some new heterocyclic aryl acetic acids and the corresponding acetohydroxamic acids and we explored their ability to inhibit soybean lipoxygenase, to present antioxidant and anti-i Read More

7-Methoxy-3-phenyl-4-phenylvinyl benzopyran-2-ones and the corresponding 2,2-dimethyl-benzopyrans, substituted with different alkylamino residues were synthesized. Except compound 13e, all compounds showed high level of estrogen agonistic activity (>81 %) whereas, compounds 13 b-e and 15a showed significant estrogen antagonistic activity (>20 %). X-Ray analysis of a 7-methoxy-3-phenyl-4-phenylvinyl benzopyra Read More

West Nile virus (WNV) is a mosquito-borne disease that emerged in North America. In 2002 it caused the largest arboviral meningoencephalitis outbreak ever recorded in the US and Canada. The key enzyme responsible for the replication of the virus is the RNA-dependent RNA polymerase (RdRp) enzyme represented by nonstructural protein NS5 in WNV To understand the structural basis and enzymatic activity of WNV RdR Read More

This study describes the design, synthesis and trypanocidal evaluation of new azaheterocyclic derivatives (4-8). These compounds were designed as megazol (1) analogs based on bioisosterism tools and were synthesized to investigate the possible pharmacophoric contribution of the 1,2,4-triazole nucleus, the position of the heterocyclic nucleus and presence of the nitro group, to the activity against the bloodstream trypomastigote Read More

The new germanium compounds of cinnamic acid, RC6H4CHGe(OCH2CH2)3NCH2COOH R=H (I), 2-OH (II), 3-OH (III), 4-OH (IV), have been obtained to study anti-tumor activities. Compounds (I-IV) were prepared by the electrophilic addition reaction and nucleophilic substitution reaction. Biological investigation has demonstrated that all compounds (I-IV) are lower toxicity with strongly anti-tumor activity than positive control.

Non-transferrin-bound iron (NTBI) is detectable in plasma of β-thalassemia patients with transfusional iron overload. This form of iron may cause oxidative tissue damage and increased iron uptake, into several vital organs. Removal of NTBI species is incomplete and transient using standard intermittent desferrioxamine (DFO) or deferiprone (DFP) monotherapy. Combinations of these or other chelators may improve the prote Read More

Among various phenolic compounds, caffeic acid (3,4-dihydroxycinnamic acid) exhibited pharmacological antioxidant, anticancer and antimutagenic activities. The antioxidant properties of phenolic compounds depend on their chemical structure, however, the role of the ethylenic side chain in the radical scavenging activity remains controversial. Thus, the aim of this study consisted to test cinnamic acid and 15 cin Read More

Endogenous opioids have been studied extensively since their discovery, in the hope of findings a perfect analgesic, devoid of the secondary effects of alkaloid opioids. However, the design of selective opioid agonists and or antagonists has proved very difficult. First, structural studies of peptides in general are hampered by their intrinsic flexibility. Second, the relationship between constitution and the socalled “bioactive conformat Read More

To find new drug candidates for treating Alzheimer's disease, we used the similarity search technique and GTS-21 as a template to search the Traditional Chinese Medicines Database. The high-score molecules thus obtained were compared with the template through the flexible alignment. Those molecules which had good alignment with GTS- 21 were selected for conducting the docking studies aimed at the α7 nicotinic ace Read More

Glucocorticoids are four-ring steroid compounds that regulate a wide range of physiological systems ranging from embryonic respiratory development, immune function and responses to acute or chronic stress. Glucocorticoids are taken up by many target cells where they bind and activate cytoplasmic glucocorticoid receptors (GRs), which then dimerize, translocate to the nucleus and function as ligand-dependent tr Read More