拓扑异构酶Ⅰ抑制剂研究进展

Developments of topoisomerase Ⅰ inhibitors in cancer chemotherapy

拓扑异构酶Ⅰ(topoisomeraseⅠ,TopoⅠ)是抗肿瘤研究的重要靶点,以TopoⅠ为靶点的药物在肿瘤化疗中被广泛应用。目前临床使用或处于临床前研究的拓扑异构酶Ⅰ抑制剂主要分为喜树碱类(camptothecin,CPT)和非喜树碱类(non-camptothecin TopoⅠinhibitor)化合物。本文主要介绍了近年来TopoⅠ抑制剂研发领域的最新进展和发展趋势,并重点就近年来涌现出的一些新的TopoⅠ抑制剂的抗肿瘤活性和药理学特性做一综述。

Following the realization that human DNA topoisomerase Ⅰ （Topo Ⅰ ） is a useful therapeutic target against tumor growth, Topo Ⅰ inhibitors represent a class of effective agents that have been extensively exploited and used for carcinoma chemotherapy. Current TopoⅠ inhibitors being clinically used or developed are classified as campotothecins and non-camptothecins. This presentation intro- duces current status and trends of Topo Ⅰ inhibitors as anti-tumor agents with an emphasis on bioactive and pharmacological properties of these agents.