Letters in Drug Design & Discovery - Volume 4, Issue 5, 2007

The investigation of metal-containing drugs over several decades has set out to improve upon the toxicity and efficacy of conventional chemotherapeutic agents. Promising pre-clinical and clinical data have fostered the broadening for the search of metal compounds in cancer treatment and combination therapy. Gallium is only second to platinum in terms of anti-tumor activity. Its subsequent investigation has b Read More

Chiral derivatives of two cyclohexylethyl halopyridyl thiourea compounds (HI-509 and HI-510), two α -methyl benzyl halopyridyl compounds (HI-511 and HI-512), and a cyclohexyl ethyl thiazolyl thiourea compound (HI-513) were synthesized and evaluated for their anti-cancer activity. Preliminary screening indicated that the (S)- isomers displayed improved activity in comparison with (R)- enantiomers to inhibit tubulin polymerizatio Read More

Synthesis of different N10-substituted-4-methyl acridones are described. The compounds are prepared with varying alkyl side chain length with propyl and butyl substitution and a tertiary amine group at the terminal end of the alkyl side chain. The structural requirement of in-vitro anti-cancer and reversal of drug resistance are studied. These compounds have been tested against the breast cancer cell lines MCF-7 and Read More

In view of the significant side-effects of existing substances as well as of supportive therapies for the treatment of pulmonary edema, there is a renewed search for novel drugs that increase the uptake of sodium in type II alveolar epithelial cells, a phenomenon which is crucial for lung liquid clearance. We describe here the discovery and characterization of a Tumor Necrosis Factor (TNF)-derived peptide mimicking the lectin-li Read More

New cisplatin analogue carrying a cholic acid, complex [PtCl(UDC)(en)] (en = ethylenediamine, UDC = Ursodeoxycholate) has been synthesized from [PtCl2(en)] and characterized. This novel complex shows increased cytotoxicity against a cisplatin-resistant ovarian tumor cell line (CH1cisR) as compared with the parent compound cisDDP. Moreover, while cisplatin only exerts its activity over the G2/M population, [PtCl(UDC)(en Read More

ERα17p is a synthetic peptide corresponding to a regulatory motif located within the autonomous AF-2a region of the estrogen receptor α (ERα). ERα17p binds to the receptor and enhances its transcriptional activity. Structural characteristics of this peptide suggest that it interferes with intra- and/or interprotein interactions involving ERα.

HIV-specific protease inhibitors are fundamental antiviral drugs for people with HIV/AIDS. Hologram quantitative structure-activity relationships (HQSAR) were conducted on a class of 82 protease inhibitors. The final model obtained was used to predict the potency of 17 test set compounds. The predicted values were in good agreement with the experimental results.

The present study examines the pharmacological profile of a new five indole derivatives 2a-e, ligands of the serotonin receptor evaluating the affinity for the serotoninergic, (5HT1A, 5HT2A and 5HT2C) receptors. The affinity of indole derivatives 2a-e (10-6-5x10-7-10-7 M) for receptors is defined as inhibition percentage of radioligand/receptor binding and measured as the radioactivity of remaining complex radioligand/rec Read More

To identify the important structural components of glutathione that induce sedative and hypnotic effects, intracerebroventricular (i.c.v.) injection of three glutathione-related dipeptides, i.e., glutamyl-cysteine (Glu-Cys), cysteinyl-glycine (Cys-Gly) and glutamyl-glycine (Glu-Gly) were given during an acute stress condition in neonatal chicks. These peptides attenuated distress vocalizations and spontaneous activity induced by social Read More

The majority of current smokers in the U.S. also have at least one comorbid psychiatric illness. Looking at commons mechanisms of nicotine dependence and psychiatric disorders of hedonic regulation reveals nicotinic acetylcholine receptors and the glycine site on NMDA receptors as potential targets for pharmacological treatment of these disorders.

The synthesis of new triphenyltin derivatives with (N-substituted-pyrazol-3-yl) carboxylic acid fragments is described. The in vitro antibacterial activity of the new agents was evaluated against two fungal strains (Saccharomyces cerevisiae and Fusarium oxysporum f.sp albedinis) and against bacterial strains (Echerichia coli). A considerable activity was recorded with respect to the three studied micro-organisms. Structure acti Read More