Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1368522 | Bioorganic & Medicinal Chemistry Letters | 2016 | 5 Pages |
Abstract
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Siliang Feng, Kuncheng Chen, Chenhong Wang, Xifeng Jiang, Huajin Dong, Zehui Gong, Keliang Liu,