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.