Review camptothecin: current perspectives.
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.
Li
Qing-Yong
QY
Key Laboratory of Forest Plant Ecology (Northeast Forestry University), Ministry of Education, Harbin 150040, China.
Zu
Yuan-Gang
YG
Shi
Rong-Zhen
RZ
Yao
Li-Ping
LP
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
D000972:Antineoplastic Agents, Phytogenic; D004791:Enzyme Inhibitors; D002166:Camptothecin