期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 1, 页码 122-127出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.10.088
关键词
Water-soluble prodrugs of paclitaxel; Self-immolative linkers; Disulfide linkers; Sulfhydryl-assisted cleavage of disulfide linkers
资金
- Piramal Enterprises management
A new series of disulfide-containing prodrugs of paclitaxel were designed, synthesized and evaluated against 6 cancer cell lines. Some of these prodrugs exhibited nearly equal or slightly better anticancer activity when compared to that of paclitaxel. These prodrugs contain water-soluble groups such as amino, carboxyl, hydroxyl, amino acids, etc., and exhibited 6-140 fold increase in aqueous solubility when compared to paclitaxel. One of these prodrugs exhibited improved water solubility, better in vitro anticancer activity and significantly superior oral bioavailability in mice when compared to those of paclitaxel. Thus, we have identified a very promising lead compound for further optimization and evaluation as a potentially bioavailable water-soluble prodrug of paclitaxel. (C) 2014 Elsevier Ltd. All rights reserved.
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