Letters in Drug Design & Discovery - Volume 5, Issue 7, 2008

Some pyrrolo[2,1-c][1,4]benzodiazepine-G1 poly (aryl ether) dendrimer hybrids have been synthesized and evaluated for their DNA binding ability as well as anticancer activity. The linkage of dendrimer component significantly increased DNA binding ability and anticancer activity apart from the enhancement of their solubility, and taking part as a drug carrier.

A new sesquiterpene lactone, 6β-O-isobutyrylbritannilactone (5) and five known sesquiterpene lactones; britannilactone (1), 1-O-acetylbritannilactone (2), Hydroxy alantolactone (3), 8-epi-ivangustin (4) and 1,6-O,Odiacetylbritannilactone (6), were isolated from the flowers of Inula britannica. In the known sesquiterpene lactones, (3) and (4) were isolated for the first time from Inula britannica. The structures of Read More

3D-QSAR analysis has been performed on a series of diaryl urea derivatives of multi-targeted receptor tyrosine kinase inhibitors. Models were developed using the most widely used computational approach molecular field analysis (MFA) from our dataset for the KDR, cKit and FLT3 inhibitors using genetic partial least square (G/PLS) method. These models showed excellent internal predictability and consistency and validation Read More

The chemical signaling like N-acylhomoserine lactones (AHLs) controlling quorum sensing (QS) processes has been emerged as a possible target for the design of a novel antimicrobial compounds. Twenty-four new N-phenylacetanoyl- L-homoserine lactones (PHLs) relative to AHLs with variable inhibition of QS were selected to develop models to establish the three-dimensional quantitative structure-activity relationships (3D-QSA Read More

A series of novel diphenyl(piperidin-4-yl)methanol derivatives 10(a-j) were synthesized and characterized by 1H NMR, LC/MS, FTIR and elemental analyses. All the compounds synthesised were evaluated for their cell antiproliferation activity by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. The antiproliferative effects of the synthesised compounds were tested against viable human skin fibr Read More

The aim of this study was to evaluate the use of a β-cyclodextrin-based polymer, and more exactly a highly crosslinked cyclodextrin-based polyester, as an excipient to accelerate the release of poorly soluble drugs from pellets obtained by extrusion-spheronisation. The cross-linked β-cyclodextrin based polymer was associated to microcrystalline cellulose to facilitate the process of extrusion/spheronisation, and nimesu Read More

Surface tension based microtensiometric method for HTS (high throughput screening) of drug solubility properties is presented. Method was tested by determining physiologically relevant parameters on the solubility of ibuprofen and indomethacin. Linear correlation was found with equilibrium solubility. According to this study, microtensiometry is a promising technique for HTS solubility testing.