ABSTRACT
A series of 2-amino-4-aryl-3-cyano-7- (dimethylamino)-4H-chromenes was synthesized by condensation of 3- (dimethylamino) phenol, an aromatic aldehyde and malonitrile in ethanol containing piperidine. The assignments of the structure of all synthesized compounds were based on spectral data (IR, Mass and(1)H NMR). The cytotoxic activities of the synthesized compounds against six human tumor cell lines were determined by MTT assay. Several compounds showed significant cytotoxic activity.
ABSTRACT
An HPLC method for determination of rofecoxib in human serum is presented. The method is based on pre-column derivatization of analyte to a phenanthrene derivative of the drug. Rofecoxib and the internal standard were extracted from serum using liquid-liquid extraction. Upon exposure to UV light, the drug was found to undergo a photocyclization reaction, giving a species with high absorbance. Validation of the method has been studied in the concentration range 10-500 ng ml(-1).
Subject(s)
Cyclooxygenase 2 Inhibitors/blood , Lactones/blood , Phenanthrenes/blood , Sulfones/blood , Calibration , Chromatography, High Pressure Liquid , Cyclization , Cyclooxygenase 2 Inhibitors/chemistry , Cyclooxygenase 2 Inhibitors/radiation effects , Humans , Lactones/chemistry , Lactones/radiation effects , Magnetic Resonance Spectroscopy , Molecular Structure , Phenanthrenes/chemistry , Phenanthrenes/radiation effects , Reference Standards , Reproducibility of Results , Sensitivity and Specificity , Sulfones/chemistry , Sulfones/radiation effects , Ultraviolet RaysABSTRACT
The chemical synthesis and physical data of several new esters of testosterone (17 beta-hydroxyandrost-4-en-3-one), which contain either a halogeno or an alkoxy substituent in the acid chain, are reported.
Subject(s)
Contraceptive Agents, Male/chemical synthesis , Testosterone/analogs & derivatives , Carboxylic Acids , Chemical Phenomena , Chemistry , Testosterone/pharmacologyABSTRACT
The synthesis of ten esters and two ethers of testosterone (17 beta-hydroxyandrost-4-en-3-one) is described. All these possess some form of alpha - and/or beta - substitution in the ester/ether side-chain. The work was undertaken in order to evaluate the long-acting antifertility effect of such compounds in males.
