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The utility of 8- Fluoro -1- Benzosuberone in synthesis of newly;Azole, pyrane and pyrimidine derivatives as cytotoxic and anti- tumor agents

W.A.Gad, D.O.Nassar

On condensation 8- fluoro-1-benzosuberone (1)with heterocyclic aldehydes affords the corresponding 2-arylidene -1-benzosuberones (2) which on treatment with malononitrile and phenylhydrazine yields the cyanoaminopyrane and pyrazole derivatives (3) and (4), respectively. Moreover, treatment of the aryl methylene (2) with thiourea gives the corresponding thioxopyrimidine derivatives (5), while using urea and guanidine hydrochloride at the similar experimental conditions leads to pyrimidinone and aminopyrimidine derivatives (6) and (7), respectively. Some of the discussed compounds showin vitro antitumor activity utilizing three human tumor cell lines, representing breast, colon as well as prostate.