Design, synthesis, and evaluation of water-soluble morpholino-decorated paclitaxel prodrugs with remarkably decreased toxicity

Feng Siliang; Chen Kuncheng; Wang Chenhong; Jiang Xifeng; Dong Huajin; Gong Zehui; Liu Keliang

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Design, synthesis, and evaluation of water-soluble morpholino-decorated paclitaxel prodrugs with remarkably decreased toxicity

机译：水溶性吗啉代修饰的紫杉醇前药的设计，合成和评估

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Novel water-soluble paclitaxel prodrugs were designed and synthesized by introducing morpholino groups through different linkers. These derivatives showed 400-20,000-times greater water solubility than paclitaxel as well as comparable activity in MCF-7 and HeLa cell lines. The prodrug PM4 was tested in the S-180 tumor mouse model, with paclitaxel as the positive control. The results showed that PM4 had comparable antitumor activity as paclitaxel, with tumor inhibition of 54% versus 56%, and remarkably decreased toxicity. The survival rate of treated mice was 8/8 in the PM4 group, compared to 3/8 in the paclitaxel group. (C) 2016 Elsevier Ltd. All rights reserved.

机译：通过不同连接基引入吗啉代基团，设计并合成了新型水溶性紫杉醇前药。这些衍生物的水溶性比紫杉醇高400-20,000倍，并且在MCF-7和HeLa细胞系中具有可比的活性。在紫杉醇作为阳性对照的S-180肿瘤小鼠模型中测试了前药PM4。结果显示，PM4具有与紫杉醇相当的抗肿瘤活性，肿瘤抑制率分别为54％和56％，并且毒性显着降低。 PM4组的治疗小鼠存活率为8/8，紫杉醇组为3/8。（C）2016 Elsevier Ltd.保留所有权利。

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《Bioorganic and Medicinal Chemistry Letters》 |2016年第15期|共5页
作者
Feng Siliang; Chen Kuncheng; Wang Chenhong; Jiang Xifeng; Dong Huajin; Gong Zehui; Liu Keliang;
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正文语种 eng
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Paclitaxel prodrugs; Morpholino group; Anticancer; Water-soluble derivatives;

机译：紫杉醇前药莫普利诺基抗癌水溶性衍生物;

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1. Design, synthesis, and evaluation of water-soluble morpholino-decorated paclitaxel prodrugs with remarkably decreased toxicity [J] . Feng Siliang, Chen Kuncheng, Wang Chenhong, Bioorganic and Medicinal Chemistry Letters . 2016,第15期

机译：水溶性吗啉代修饰的紫杉醇前药的设计，合成和评估
2. A Novel Approach of Water-Soluble Paclitaxel Prodrug with No Auxiliary and No Byproduct: Design and Synthesis of Isotaxel [J] . Yoshio Hayashi, Mariusz Skwarczynski, Yoshio Hamada, Journal of Medicinal Chemistry . 2003,第18期

机译：无助剂，无副产物的水溶性紫杉醇前药的新方法：异紫杉醇的设计与合成
3. Synthesis and evaluation of water-Soluble paclitaxel prodrugs. [J] . Feng X, Yuan YJ, Wu JC Bioorganic and Medicinal Chemistry Letters . 2002,第22期

机译：水溶性紫杉醇前药的合成与评价。
4. Spontaneously regenerable water-soluble prodrugs:application to HIV protease inhibitors and anti-cancer drug paclitaxel [C] . Youhei Sohma, Hikaru Matsumoto, Masato Sasaki, European Peptide Symposium . 2002

机译：自发性可再生水溶性前药：在HIV蛋白酶抑制剂和抗癌药物紫杉醇的应用
5. Design, synthesis, biological evaluation and molecular modeling of novel taxane-based anticancer agents and paclitaxel mimics. [D] . Sun, Liang. 2008

机译：新型紫杉烷类抗癌药和紫杉醇模拟物的设计，合成，生物学评估和分子建模。
6. Design Synthesis and Biological Evaluation of Water-Soluble Amino Acid Prodrug Conjugates Derived from Combretastatin Dihydronaphthalene and Benzosuberene-Based Parent Vascular Disrupting Agents [O] . Laxman Devkota, Chen-Ming Lin, Tracy E. Strecker, -1

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7. Prodrug of Antitumor Agents : Design and synthesis of Water-soluble derivative [O] . 原田直之, Harada Naoyuki, ハラダナオユキ 100

机译：抗肿瘤药物的前药：水溶性衍生物的设计和合成

Design, synthesis, and evaluation of water-soluble morpholino-decorated paclitaxel prodrugs with remarkably decreased toxicity

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