Water soluble camptothecin derivative and medicinal composition containing same

A technology of camptothecin and derivatives, applied in the field of medicine based on camptothecin, can solve the problem of not being used as a CPT prodrug and the like, and achieve the effects of improving stability and reducing drug toxicity
CN102153607AActive Publication Date: 2011-08-17HUNAN FANGSHENG PHARMACEUTICAL CO LTD

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

The invention relates to a water soluble derivative of camptothecin and a preparation method thereof. The derivative has a structure shown in a formula (I). The derivative of the camptothecin has improved anticancer activity.
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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...

Claims

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