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camptothecin
Camptothecin (CPT) is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoisomerase I (topo I). It was discovered in 1966 by M. E. Wall and M. C. Wani in systematic screening of natural products for anticancer drugs. It was isolated from the bark and stem of ''Camptotheca acuminata'' (Camptotheca, Happy tree), a tree native to China used as a cancer treatment in Traditional Chinese Medicine.〔. the stem bark of Mappia foetida , a tree native to India, has proved to be another source significant for the isolation of camptothecin.TR Govindachari and N. Viswnathan, Phytochemistry,11(12), 3529-31 (1972)).
〕 CPT showed remarkable anticancer activity in preliminary clinical trials but also low solubility and (high) adverse drug reaction. Because of these disadvantages synthetic and medicinal chemists have developed numerous syntheses of Camptothecin and various derivatives to increase the benefits of the chemical, with good results. Two CPT analogues have been approved and are used in cancer chemotherapy〔Takimoto CH, Calvo E. ("Principles of Oncologic Pharmacotherapy" ) in Pazdur R, Wagman LD, Camphausen KA, Hoskins WJ (Eds) (Cancer Management: A Multidisciplinary Approach ). 11 ed. 2008.〕 today, topotecan and irinotecan.
==Structures==
CPT has a planar pentacyclic ring structure, that includes a pyrrolo()-quinoline moiety (rings A, B and C), conjugated pyridone moiety (ring D) and one chiral center at position 20 within the alpha-hydroxy lactone ring with (S) configuration (the E-ring). Its planar structure is thought to be one of the most important factors in topoisomerase inhibition.
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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