T. Yamaguchi et al., Synthesis of taxoids 5. Synthesis and evaluation of novel water-soluble prodrugs of a 3 '-desphenyl-3 '-cyclopropyl analogue of docetaxel, BIOORG MED, 9(12), 1999, pp. 1639-1644
A novel 3'-desphenyl-3'-cyclopropyl analogue of docetaxel was synthesized f
rom 10-deacetylbaccatin III. The cytotoxicity of the new taxoid was evaluat
ed against several human tumor cell lines, and it had ca. 20 times stronger
activity against human colon cancer cell lines (WiDr and Colon 320) than t
hat of docetaxel. This taxoid was converted to its water-soluble prodrugs t
hat have 2'-substituted amino acid derivatives with spacer. The prodrugs ha
d good solubility in saline and showed more potent antitumor activity again
st B16 melanoma in mice than that of docetaxel. (C) 1999 Elsevier Science L
td. All rights reserved.