M. Noolvi, H. Patel
2013
Citations
0
Influential Citations
32
Citations
Quality indicators
Journal
Arabian Journal of Chemistry
Abstract
Abstract A novel 3-(substituted benzylideneamino)-7-chloro-2-phenyl quinazoline-4(3 H )-one ( 7 – 27 ) has been synthesized and characterised by IR, 1 H NMR, 13 C NMR spectroscopy, and elemental analysis. We changed the methodology for the synthesis of 3-amino 7-chloro-2-phenyl quinazolin-4(3 H )-one 6 to fusion reaction at 250 °C, instead of using solvent, to avoid the problem of ring opening, which is commonly observed while synthesizing quinazolines from benzoxazinone. NCI selected, 7-chloro-3-{[(4-chlorophenyl) methylidene] amino}-2-phenylquinazolin-4(3 H )-one 12 , with GI 50 value of −5.59 M, TGI value of −5.12 M, and LC 50 value of −4.40 M showed remarkable activity against CNS SNB-75 Cancer cell line. Rational approach and QSAR techniques enabled the understanding of the pharmacophoric requirement for 2,3,7-tri substituted quinazoline derivatives to inhibit EGFR-tyrosine kinase as antitumor agents and could be used as an excellent framework in this field that may lead to discovery of potent anti tumor agent.