Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents

作者: Qingqing Huang , Lei Wang , Wei Lu

DOI: 10.1016/J.EJMECH.2013.01.058

关键词:

摘要: Camptothecin (CPT), a natural topoisomerase (Topo) I inhibitor, exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers. However, the poor solubility inherent instability of lactone E-ring in physiological pH resulted low therapeutic efficacy severe toxicity. In past several decades' substantial progress toward understanding its pharmacology, lots analogs have been prepared to overcome drawbacks. The review provides detailed discussion evolution medicinal chemistry CPT with modification lactone.

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