[A symphony for the camptothecins]

Bull Cancer. 2003 Mar;90(3):239-45.
[Article in French]

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.

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / therapeutic use
  • Camptothecin / analogs & derivatives*
  • Camptothecin / chemistry
  • Camptothecin / therapeutic use
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / therapeutic use
  • Irinotecan
  • Music
  • Neoplasms / drug therapy*
  • Organosilicon Compounds / chemistry
  • Organosilicon Compounds / therapeutic use
  • Structure-Activity Relationship
  • Topoisomerase I Inhibitors*
  • Topotecan / chemistry
  • Topotecan / therapeutic use

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Organosilicon Compounds
  • Topoisomerase I Inhibitors
  • cositecan
  • 7-tert-butyldimethylsilyl-10-hydroxycamptothecin
  • lurtotecan
  • Irinotecan
  • Topotecan
  • rubitecan
  • exatecan
  • Camptothecin