Synthesis of long-circulating, backbone degradable HPMA copolymer-doxorubicin conjugates and evaluation of molecular-weight-dependent antitumor efficacy.

Synthesis of long-circulating, backbone degradable HPMA copolymer-doxorubicin conjugates and evaluation of molecular-weight-dependent antitumor efficacy.
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长循环的,可降解的HPMA共聚物 - 道霉素结合物的合成以及分子量依赖性抗肿瘤功效的评估。

DOI:
10.1002/mabi.201200353
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发表时间:
2013-02
影响因子:
4.6
通讯作者:
Kopeček J
Kopeček J
中科院分区:
工程技术3区
文献类型:
--
作者:
Pan H;Sima M;Yang J;Kopeček J

文献摘要

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Backbone degradable, linear, multiblock N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer–doxorubicin (DOX) conjugates are synthesized by reversible addition–fragmentation chain transfer (RAFT) polymerization followed by chain extension via thiol-ene click reaction. The examination of molecular-weight-dependent antitumor activity toward human ovarian A2780/AD carcinoma in nude mice reveals enhanced activity of multiblock, second-generation, higher molecular weight conjugates when compared with traditional HPMA copolymer–DOX conjugates. The examination of body weight changes during treatment indicates the absence of non-specific adverse effects.