title: [A symphony for the camptothecins].
abstract: Cancer occurs and it is life that runs off the rails. To restore the melody, the oncologist can use an array of pharmacological instruments which he needs to tune optimally to reach the maximal efficacy. Camptothecin derivatives, inhibitors of topoisomerase I, represent an essential family of the chemotherapeutic arsenal. Topotecan and irinotecan have been used in the clinic for a number of years, but other potent analogues are appearing and broaden the range of topoisomerase I poisons. In this review, we present the main molecular characteristics of the second generation of camptothecins (lurtotecan, exatecan, rubitecan, silatecan). The future is also evoked with camptothecin derivatives bearing a modified lactone ring, in particular the homocamptothecins and the drug diflomotecan, which shows promise as an anticancer. The camptothecin partition is disclosed here.
authors.affiliation: Laboratoire de pharmacologie antitumorale, Centre Oscar-Lambret, Unité 524 Inserm, place de Verdun, 59045 Lille.
authors.forename: Amélie
authors.initials: A
authors.lastname: Lansiaux
authors.forename: Christian
authors.initials: C
authors.lastname: Bailly
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000627:therapeutic use; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000627:therapeutic use; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000627:therapeutic use; D000077146:Irinotecan; D009146:Music; D009369:Neoplasms / Q000188:drug therapy*; D017646:Organosilicon Compounds / Q000737:chemistry / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors; D019772:Topotecan / Q000737:chemistry / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D017646:Organosilicon Compounds; D059004:Topoisomerase I Inhibitors; C406143:cositecan; C415575:7-tert-butyldimethylsilyl-10-hydroxycamptothecin; C091719:lurtotecan; D000077146:Irinotecan; D019772:Topotecan; C079905:rubitecan; C095887:exatecan; D002166:Camptothecin