Water soluble camptothecin derivative and medicinal composition containing same
Patent Information
- Authority / Receiving Office
- CN Β· China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- HUNAN FANGSHENG PHARMACEUTICAL CO LTD
- Publication Date
- 2011-08-17
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Abstract
Description
technical field
[0001] The present invention relates to the field of medicine, more specifically to the field of anticancer drugs, and more specifically to camptothecin-based drugs. Background technique
[0002] Camptothecin (CPT), a cytotoxic alkaloid, was first isolated by Wall and colleagues from the leaves and bark of a plant native to China, Camptotheca accuminata, Nyssaceae Validation (J. Am. Chem. Soc. 88, 3888, 1966). The major cellular target of CPT is topoisomerase I (topo I), an enzyme involved in the relaxation of supercoiled chromosomal DNA by transient single-strand cleavage, unwinding, and religation of double DNA during DNA replication. CPT binds at the interface of the covalent binary topo I-DNA complex, forming a stable ternary complex that prevents religation, thus leading to replication-mediated double-strand breaks and DNA damage. Because CPT inhibition can lead to cell death in the S phase of the cell cycle, CPT has become a focus of intensive researc...