| Literature DB >> 17485207 |
Carlo Ballatore1, Edward Hyde, Robert F Deiches, Virginia M-Y Lee, John Q Trojanowski, Donna Huryn, Amos B Smith.
Abstract
A series of paclitaxel C-10 carbamates was synthesized and evaluated in a bi-directional permeability assay in comparison with paclitaxel and the blood-brain barrier-permeable C-10 ester derivative, TX-67. A number of the carbamates were found not to be substrates for Pgp. Moreover, when tested for Pgp-inhibitory potential, representative compounds proved to be devoid of Pgp interactions. Side-by-side comparison between TX-67 and the corresponding C-10 carbamate, CNDR-3, revealed a significantly longer half-life for CNDR-3 in both mouse and human plasma, suggesting that this class of derivatives is appropriate for further in vivo evaluation.Entities:
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Year: 2007 PMID： 17485207 PMCID： PMC2648301 DOI： 10.1016/j.bmcl.2007.04.058
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823