Synthesis and antitumor activity of novel C-8 ester derivatives of leinamycin
Synthesis and antitumor activity of novel C-8 ester derivatives of leinamycin
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DOI：
10.1016/s0960-894x(02)00949-6
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发表时间：
2003-02-10
影响因子：
2.7
通讯作者：
Tamaoki, T
中科院分区：
文献类型：
--
作者：
Kanda, Y;Ashizawa, T;Tamaoki, T
本发明描述了一系列新的来那霉素C-8酯衍生物。通过N-取代氨基酸或含聚醚基团的羧酸与莱那霉素的缩合反应，合成了具有良好抗肿瘤活性的C-8酯类衍生物。在这些衍生物中，在C-8酰基中具有五个乙二醇醚单元的化合物4 e对人肿瘤异种移植物显示出有效的抗肿瘤活性。结合二硫戊环酮部分的修饰应用于这些C-8酯衍生物，其中一些也显示出良好的抗肿瘤活性。(C)2002爱思唯尔科技有限公司版权所有。
A novel series of C-8 ester derivatives of leinamycin are described. Condensation of N-substituted amino acids or carboxylic acids containing polyether moiety with leinamycin resulted in the C-8 ester derivatives with good antitumor activity in several experimental models. Among these derivatives, compound 4e, which has five ethylene glycol ether units in the C-8 acyl group, showed potent antitumor activity against human tumor xenograft. Combination with the modification of the dithiolanone moiety was applied to these C-8 ester derivatives and some of them also showed good antitumor activity. (C) 2002 Elsevier Science Ltd. All rights reserved.