Synthesis and biological evaluation of new camptothecin derivatives obtained by modification of position 20
Synthesis and biological evaluation of new camptothecin derivatives obtained by modification of position 20
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DOI：
10.1016/j.bmc.2010.09.069
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发表时间：
2010-12-15
影响因子：
3.5
通讯作者：
Passarella, Daniele
中科院分区：
文献类型：
--
作者：
Riva, Elena;Comi, Daniela;Passarella, Daniele
描述了一系列新型二聚喜树碱衍生物的制备和生物学评价。所有新化合物均显示出显着的抑制人肿瘤细胞生长的能力，IC50值范围为0.03至12.2μM。对核酶拓扑异构酶活性的干扰已被证明，突出了所获得的副产物之一对拓扑异构酶I的毒害作用。所获得的化合物之一已被证明具有中等的抗血管生成活性。此外，还在转基因小鼠细胞上研究了四种新化合物对半胱天冬酶活性和ROS生成的影响。 (C) 2010 Elsevier Ltd. 保留所有权利。
The preparation and biological evaluation of a novel series of dimeric camptothecin derivatives are described. All the new compounds showed a significant ability to inhibit human tumor cell growth with IC50 values ranging from 0.03 to 12.2 mu M. The interference with the activity of the nuclear enzymes topoisomerases has been demonstrated, highlighting the poison effect of one of the obtained byproducts toward topoisomerase I. A moderate antiangiogenic activity has been demonstrated for one of the obtained compounds. Moreover, the effects of four new compounds on caspases activity and ROS generation have been studied on transgenic mouse cell. (C) 2010 Elsevier Ltd. All rights reserved.