Stable and orally bio-available pro-drugs of CPS11

Aihong Huo; Hesheng Zhang; Yongbiao Guan; Guanghuai Zeng; Yingwei Chen; Xingwen Li

doi:10.1016/j.bmcl.2011.09.026

Stable and orally bio-available pro-drugs of CPS11

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6242-4. doi: 10.1016/j.bmcl.2011.09.026. Epub 2011 Sep 13.

Authors

Aihong Huo¹, Hesheng Zhang, Yongbiao Guan, Guanghuai Zeng, Yingwei Chen, Xingwen Li

Affiliation

¹ Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China.

PMID: 21963304
DOI: 10.1016/j.bmcl.2011.09.026

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.

MeSH terms

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
Prodrugs / pharmacokinetics*
Thalidomide / analogs & derivatives*
Thalidomide / pharmacokinetics
Thalidomide / pharmacology
Umbilical Veins / cytology
Umbilical Veins / drug effects
Xenograft Model Antitumor Assays

Substances

CPS 11
Prodrugs
Thalidomide