title: Heteroannelation of Cyclic Ketones: Synthesis, Characterization and Antitumor Evaluation of Some Condensed Azine Derivatives.
abstract: A series of pyrimidine and thiazine derivatives was synthesized by one-pot reaction of cyclopentanone with a mixture of an aromatic aldehyde, namely o-anisaldehyde, and different ureas, namely urea, guanidine and thiourea, respectively. Furthermore, cycloaddition reaction of active methylene reagents, namely acetyl acetone, malononitrile, ethyl cyanoacetate, cyanoacetamide and N-phenyl cyanoacetamide with 2,6-bis(2-methoxybenzylidene)cyclohexanone afforded chromene and quinoline derivatives in basic medium. The antitumor evaluation of some new compounds against three human cell lines, namely MCF-7, NCI-H460 and SF-268 showed significant and moderate activity compared with the positive control doxorubicin.
authors.forename: A Essam
authors.initials: AE
authors.lastname: Soylem
authors.forename: G Mohammed
authors.initials: GM
authors.lastname: Assy
authors.forename: M Ghania
authors.initials: MG
authors.lastname: Morsi
mesh_terms: D045744:Cell Line, Tumor; D003500:Cyclization; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007659:Ketones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D066244:Proton Magnetic Resonance Spectroscopy
chemical_list: D007659:Ketones