Diarylsemicarbazones: synthesis, antineoplastic activity and topoisomeraseI inhibition assay

A series of diarylsemicarbazones was synthesized and tested against human n eoplastic cell lines. The more active members have a 1-naphthyl ring at the carbamidic nitrogen, and chloro, dimethylamino or nitro group substituents at the benzylidene moiety. None of these showed affinity to DNA. One of th e more active compounds was tested as a topoisomerase I inhibitor and showe d a potent effect. SAR studies demonstrated linear correlation between lypo philicity and activity on the most sensitive lines and a definite conformat ional shape for antineoplastic action. (C) 1999 Elsevier Science S.A. All r ights reserved.