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Stable and orally bio-available pro-drugs of CPS11.
Huo, Aihong; Zhang, Hesheng; Guan, Yongbiao; Zeng, Guanghuai; Chen, Yingwei; Li, Xingwen.
Bioorg Med Chem Lett ; 21(21): 6242-4, 2011 Nov 01.
Article in English | MEDLINE | ID: mdl-21963304

ABSTRACT

Stable and orally bio-available pro-drugs of CPS11 were synthesized. They are active on human umbilical vein endothelial cell proliferation assay and tube formation assay. The therapeutic efficacy and safety of 4 as a single agent or combined with Taxol in the treatment of MX-1 human breast cancer xenograft were evaluated. Compound 4 as a single agent failed to produce an anti-tumor activity, while it significantly enhanced antitumor potency of Taxol.


Subject(s)
Prodrugs/pharmacokinetics , Thalidomide/analogs & derivatives , Biological Availability , Cell Proliferation/drug effects , Cells, Cultured , Chromatography, High Pressure Liquid , Drug Screening Assays, Antitumor , Drug Stability , Endothelium, Vascular/cytology , Endothelium, Vascular/drug effects , Female , Humans , Thalidomide/pharmacokinetics , Thalidomide/pharmacology , Umbilical Veins/cytology , Umbilical Veins/drug effects , Xenograft Model Antitumor Assays
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