Abstract
Efficient syntheses of two taxol analogs bearing the linear polyamine spermine at 7- and 10-positions of paclitaxel and 10-deacetyl-paclitaxel have been developed. These polyamine-taxol-conjugates were isolated as water soluble difluoride salts. The aim of the present work was to introduce a chemical modification into taxol skeleton in order to increase drug selectivity toward tumor cells. The cytotoxic activity of these conjugates was evaluated in MCF7 and MCF7-R cell lines. The observed low cytotoxicity suggests that these conjugates could act as potential prodrugs.
Original language | English (US) |
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Pages (from-to) | 2667-2670 |
Number of pages | 4 |
Journal | Tetrahedron Letters |
Volume | 47 |
Issue number | 16 |
DOIs | |
State | Published - Apr 17 2006 |
Keywords
- Antitumor
- Paclitaxel
- Prodrug conjugates
- Spermine
ASJC Scopus subject areas
- Biochemistry
- Drug Discovery
- Organic Chemistry