title: Review camptothecin: current perspectives.
abstract: The review provides a detailed discussion of recent advances in the medicinal chemistry of camptothecin, a potent antitumor agent that targets topoisomerase I. Thousands of CPT derivatives have been synthesized. Two of them, Topotecan and Irinotecan, are commercially approved for use in clinic as antitumor agents while more are still in clinic trials. This review summarizes the current status of the modern synthetic approaches to CPT, the mechanism of action of CPT, the structure-activity relationship(SAR), a number of novel CPT analogs and their biologic activity. There is a systematic evaluation of A-, B- and E-ring- modified camptothecins reported recently.
authors.affiliation: Key Laboratory of Forest Plant Ecology (Northeast Forestry University), Ministry of Education, Harbin 150040, China.
authors.forename: Qing-Yong
authors.initials: QY
authors.lastname: Li
authors.forename: Yuan-Gang
authors.initials: YG
authors.lastname: Zu
authors.forename: Rong-Zhen
authors.initials: RZ
authors.lastname: Shi
authors.forename: Li-Ping
authors.initials: LP
authors.lastname: Yao
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002166:Camptothecin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000032:analysis / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004791:Enzyme Inhibitors; D002166:Camptothecin