Paclitaxel analogues from Taxus x media cv. Hicksii.

The roots of T. x media Rehd. cv. Hicksii gave three novel analogues of paclitaxel modified at the N-acyl residue (N-debenzoyl-N-alpha-methylbutyryl paclitaxel and N-debenzoyl-N-cinnamoyl paclitaxel, 1b and 1c, respectively) or at the ester group at C-2 (2-debenzoyl-2-tigloyl paclitaxel, 1d). Compounds 1b and 1d showed reduced cytotoxicity and tubulin binding compared to paclitaxel, while 1c retained substantial activity in these assays.