Antitumour drug design: DNA-binding ligands, which inhibit the topoisomerase I.
DNA-enzymes, which are overexpressed in special tumour cells represent in general interesting targets for an antitumour drug design. In this context a survey about the function and the biochemical mechanistic aspects of topoisomerases is given. In the last years detailed studies in medicinal chemistry (structure activity relationships) revealed that first of all topoisomerase I inhibitor will become an attractive class of promising and perhaps more selective drugs in cancer chemotherapy. Thus, in the present review actual aspects about drug design developments of topoisomerase I inhibitors are presented. Moreover some recent results about new lead substances, some structure activity relationships and some clinical aspects are discussed.
Pindur
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U
Institute of Pharmacy, Faculty of Chemistry and Pharmacy, University of Mainz, Germany.
Lemster
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T
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004264:DNA Topoisomerases, Type I / Q000737:chemistry; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D059004:Topoisomerase I Inhibitors
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D059004:Topoisomerase I Inhibitors; D004264:DNA Topoisomerases, Type I