Abstract
The present review concentrates on camptothecin (CPT) analogues, the most extensively studied topoisomerase I (topo I) inhibitors, and provides concise information on the structural features of human topo I enzyme, mechanisms of interaction of CPT with topo I, structure-activity relationship study of CPT analogues including the influence of lactone stability on antitumor activity, and recent updates of valuable CPT analogues.
Keywords: topoisomerase, camptothecin, structural features of human topo enzyme, structure-activity relationship, monomeric protein, lurtotecan, rubitecan, highly lipophilic