SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL C-4 AZIRIDINE-BEARING PACLITAXEL (TAXOL) ANALOGS

Three novel C-4 aziridine-bearing paclitaxel analogs, 3-5, have been s ynthesized during the course of our continuing effort at C-4 modificat ion. The key step in the synthesis is the aziridine ring formation at the C-4 position via an intramolecular Mitsunobu reaction. The synthes es and the biological evaluation of these C-4 aziridine-containing der ivatives are herein discussed.