Letters in Drug Design & Discovery - Volume 8, Issue 4, 2011

The 4-diethylaminomethylbenzyl-substituted titanocene dichloride (Titanocene Y*), which is completely water- soluble and showed nanomolar activity against the human renal cancer cells CAKI-1, was tested in vitro in an antiangiogenesis assay against human umbilical vein endothelial cells, HUVEC, delivering an IC50 value of 23 +/- 17 μM. Titanocene Y* was then given at 25, 50 and 75 mg/kg/d, on five consecutive days per Read More

A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studyin Read More

Four (6,7-dimethoxy-2-oxo-2H-chromen-4-yl)methyl 3-arylacrylate (5a-d) analogues of the antitumor agent (6,7-dimethoxy-2-oxo-2H-chromen-4-yl)methyl 3-(4-methoxyphenyl)acrylate (2) were synthesized. The compounds 5a-d have one or two nitrogen atoms incorporated on the aryl moiety, and therefore could be converted into hydrochloride salts (6a-d) and these salts possess greater water solubility compared to 2. Read More

Quinoxaline-2, 3-dione obtained from cyclocondensation reaction of o-phenylene diamine with oxalic acid, was reacted with chlorosulphonic acid under cold condition followed by a reaction with various benzimidazoles to give 2, 3- dioxo-1, 2, 3, 4-tetrahydroquinoxaline-6-sulphonyl benzimidazoles in satisfactory yield. Their structures were confirmed using 1H NMR, IR and mass analysis. Cytotoxicity of these derivativ Read More

Purpose: Vagus Nerve Stimulation (VNS) is indicated in the treatment of pharmacoresistant epilepsy. Albeit its general efficacy, the use of VNS remains undefined concerning two points: i) there are only a few long-term studies, none randomized; ii) there are no clinical markers which allow to predict VNS response. In order to explore these points, we report the long-term outcomes of VNS in 22 patients. Methods: Twenty-two Read More

A novel synthetic procedure for a series of 4-Aryl-3-phenyl-6,7,8,9-tetrahydro- benzothieno[3,2- f][1,4]oxazepin-5(4H)-one 8a-s derivatives had been described. Six compounds 8a,b,h,j,m,s were selected and submitted to pharmacological evaluation for anxiolytic activity in the open field test. All the test compounds except 8b significantly reduced the exploratory activity and the emotionality of the rats in the open-field. These i Read More

The mammalian target of rapamycin (mTOR) has become an attractive target for the treatment of cancer. A computational strategy based on comparative molecular fields analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) followed by molecular docking studies was performed on a series of 4- morpholinopyrrolopyrimidine derivatives and used to identify the most important features impa Read More

Apoptosis, the programmed cell death, is a highly organized process essential for elimination of degenerated cells. Therefore, a tremendous effort is put into the development of new cancer therapeutics, which induce apoptosis in tumor cells. The integration of novel computer-based strategies, which accelerate this development, is a challenging goal. In this context, a variety of terphenyl-based compounds that mimic the alpha- Read More

Lymphatic Filariasis is a dreadful disease of mankind that infects more than one billion people worldwide. It is mainly caused by the nematode worms Wuchereria bancrofti, Brugia malayi and Brugia timori. Antifilarial agents that can kill all the stages in the life cycle of causative filariae are yet to be developed. Trehalose phosphatase is one of the key enzymes that plays a vital role in trehalose metabolism important for egg Read More

We report in this work the antimalarial activity of N-dodecyl-ethylenediamine (NDEDA). This compound was tested in vivo in a Plasmodium berghei murine model using the 4-day suppressive test in two separate experiments and displayed a very good inhibition of parasite multiplication.

A number of new derivatives of monoterpenoid with a para-menthane framework 3-methyl-6-(prop-1-en-2- yl)cyclohex-3-ene-1,2-diol (-)-3 were synthesized. The antiviral activity of (-)-3 and its derivatives against the pandemic influenza virus A/California/07/09 (H1N1)v was studied in vitro. Compound (-)-3 was found to be active against this virus (selectivity index 7.5); for mononicotinate (+)-6 the selectivity index was 17. Th Read More

The effective management of the cutaneous herpes simplex virus infections with acyclovir sodium (ACV) is limited due to reduced availability of ACV at the basal epidermis. The present research focused to improve the transcutaneous permeation of ACV from carbopol gels with different chemical permeation enhancers (dimethylsulfoxide, dlimonene, sodium taurodeoxycholate). The ex-vivo permeation was carried out usi Read More

Lipid peroxidation is the oxidative modification of polyunsaturated fatty acids (PUFA) that leads to hydroperoxides. Hydroperoxides that are derived from the lipid arachidonic acid serve as regulators of the enzymes involved in prostaglandin synthesis. Further oxidation of these hydroperoxides produces short chain aldehydes, such as 4- hydroxynonenal. The mechanism of lipid peroxidation is well established, yet it is difficult to p Read More