ABSTRACT
Pharmacophore mapping investigations were carried out on a dataset of 36 pyrazole derivatives that demonstrate antiproliferative activity in human ovarian adenocarcinoma A2780 cells. Pharmacophore modeling is a powerful tool for activity prediction of the ligands. Three point pharmacophore model was developed with two hydrophobic groups, one hydrogen bond acceptor, as pharmacophoric features. The pharmacophore hypothesis AHH.14 with R[2] value 0.909 yields a 3D-QSAR model which is statistically significant and best pharmacophore hypothesis. External validation of AHH.14 was performed by activity prediction of test set molecules with squared predictive correlation coefficient of 0.875 was observed between experimental and predicted activity values of test set molecules. AHH.14 pharmacophore model may offer potential for the design of antiproliferative agents via development of lead structures
Subject(s)
Cell Proliferation/drug effects , Quantitative Structure-Activity RelationshipABSTRACT
We report a case of idiopathic tubulointerstitial nephritis associated with bilateral uveitis(TINU syndrome) in an elderly lady,who with non-specific systemic associations developed acute renal failure,is described to increase awareness of the condition and also suggest a change in The Royal College of Ophthalmologists guidelines on Investigation of patients with Uveitis'.KEYWORDS: Idiopathic tubulointerstitial nephritis associated with bilateral uveitis; renal failure; guidelines; uveitis