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1. GIMATECAN
[A semisynthetic, lipophilic derivative of camptothecin, a quinoline alkaloid extracted from the Asian tree Camptotheca acuminate, with potential antineoplastic activity. Gimatecan binds to and inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA. This inhibits the religation of topoisomerase I-mediated single-stranded DNA breaks and produces potentially lethal double-stranded DNA breaks when encountered by the DNA replication machinery. This results in an inhibition of DNA replication and a subsequent induction of apoptosis. Gimatecan exhibits anti-angiogenic effect by mechanisms that have yet to be fully elucidated, but this agent appears to prevent the mobility of endothelial cells, and inhibits the expression of the proangiogenic basic fibroblast growth factor (bFGF). ( NCI )] (UMLS (NCI) C1455513) =Organic Chemical; Pharmacologic Substance ;

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