|
Heterocyclic Letters 2013
SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL N-(SUBSTITUTED BENZYL)-N-PROPYL-2-(TRICHLOROMETHYL) QUINAZOLIN-4-AMINE DERIVATIVES AS CYTOTOXIC AGENTS Synthese und biologische Evaluierung neuartiger N-(SUBSTITUIERTEN BENZYL)-N-propyl-2-(trichlormethyl) chinazolin-4-amin DERIVATE ALS zytotoxischen WirkstoffenKeywords: Cytotoxicity, 2-trichlomethyl quinazoline, MTT assay, A549 cell lines, HT-29 cell lines Abstract: A series of novel 2-trichloromethyl quinazoline derivatives bearing tertiary amine group at the 4th position were synthesized and evaluated for their in-vitro cytotoxicity against human lung carcinoma cell line A549 and Human colorectal adernocarcinoma cell line HT-29 by MTT assay method. All the molecules were designed on the basis of Hydrogen bond acceptor, trichloro methyl group and presence of aromatic ring. The targeted compounds (8a-o) were synthesized from 4-chloro-2-(trichloromethyl) quinazolines and N-(substituted benzyl) propan-1-amines in alcoholic medium under reflux for 15-18 h. Compounds 8f and 8l exhibited highest cytotoxicity against human lung carcinoma A549 cell line (IC50 7.5 and 6.8 G) and human colon carcinoma HT-29 cell line (IC50 8.2 and 8.0 G) among the derivatives
|