Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Organic Chemistry

This thesis includes four chapters. The first chapter is an introduction which includes a survey about topoisomerase enzymes, their inhibitors and the synthesis of quinolines and 1,8-naphthyridine derivatives. The second chapter shows the objectives of the work and the designed schemes required for the preparation of the target compounds. The third chapter includes the theoretical discussion of the experimental work, cytotoxic activity, cell cycle analysis and topoisomerase II{uF061} inhibitory activity. Furthermore, it discusses the molecular modeling for all synthesized compounds and the standard topoisomerase II inhibitor merbarone. The fourth chapter studies the experimental part of this thesis which contains the procedures used for the synthesis of the starting compounds, the target compounds and intermediates as well as the physical properties of the synthesized compounds, elemental analysis and spectral data. In addition, it demonstrates the results and procedures for the cytotoxic activity, cell cycle analysis and topoisomerase II{uF061} inhibitory activity as well as the molecular modeling study

Issued also as CD