Antitumor agents.: Part 227:: Studies on novel 4′-O-demethyl-epipodophyllotoxins as antitumor agents targeting topoisomerase II
Antitumor agents.: Part 227:: Studies on novel 4′-O-demethyl-epipodophyllotoxins as antitumor agents targeting topoisomerase II
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DOI：
10.1016/j.bmc.2004.03.067
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发表时间：
2004-06-15
影响因子：
3.5
通讯作者：
Lee, KH
中科院分区：
文献类型：
--
作者：
Xiao, ZY;Bastow, KF;Lee, KH
合成并评价了8个新的表鬼臼毒素衍生物(6-13)，旨在克服耐药性和增强拓扑异构酶II的抑制作用。其中两个化合物(7和8)与原型分子依托泊苷(1)相比，表现出更好的临床前活性，包括细胞生长抑制、细胞杀伤和体外拓扑异构酶II抑制。他们还保留了GL-331(4)的优异耐药性，GL-331(4)是一种目前正在进行临床评估的表鬼臼毒素衍生物。(C)2004爱思唯尔有限公司。保留所有权利。
Eight novel epipodophyllotoxin derivatives (6-13), which were designed to overcome drug resistance and enhance topoisomerase II inhibition, were synthesized and evaluated. Two of these compounds (7 and 8) showed better preclinical activity profiles, including cell growth inhibition, cell killing, and in vitro topoisomerase II inhibition, as compared to the prototype molecule etoposide (1). They also retained the superior drug-resistance profile of GL-331 (4), an epipodophyllotoxin derivative currently in clinical evaluation. (C) 2004 Elsevier Ltd. All rights reserved.