Sriram Dharmarajan, Yogeeswari Perumal, Thirumurugan Rathinasabapathy, Bal Tanushree Ratan
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani 333 031, India.
Nat Prod Res. 2005 Jun;19(4):393-412. doi: 10.1080/14786410412331299005.
Topoisomerase I (Topo-I) is a major target for anticancer drug discovery and design. As a result, Topo-I inhibitors constitute an important class of the current anticancer drugs. To date, all of the Topo-I inhibitors that have been clinically evaluated are analogues of camptothecin (CPT), an extract of the Chinese tree Camptotheca acuminata. CPT has shown significant antitumor activity to lung, ovarian, breast, pancreas and stomach cancers. In this article the, phytochemical aspect, and various structural modifications are comprehensively reviewed as in rings A, B, C, D and E. Biological activity of camptothecin, other than anticancer, reported till the year 2003 has also been discussed.
拓扑异构酶I(Topo-I)是抗癌药物研发的主要靶点。因此,Topo-I抑制剂是目前抗癌药物的重要类别。迄今为止,所有经过临床评估的Topo-I抑制剂都是喜树碱(CPT)的类似物,CPT是中国植物喜树的提取物。CPT对肺癌、卵巢癌、乳腺癌、胰腺癌和胃癌显示出显著的抗肿瘤活性。本文全面综述了喜树碱在A、B、C、D和E环方面的植物化学特性以及各种结构修饰。还讨论了截至2003年报道的喜树碱除抗癌之外的生物活性。