178248-34-5Relevant articles and documents
Synthesis of taxoids 5. Synthesis and evaluation of novel water-soluble prodrugs of a 3'-desphenyl-3'-cyclopropyl analogue of docetaxel
Yamaguchi, Tetsuo,Harada, Naoyuki,Ozaki, Kunihiko,Arakawa, Hiroaki,Oda, Kouji,Nakanishi, Noriyuki,Tsujihara, Kenji,Hashiyama, Tomiki
, p. 1639 - 1644 (2007/10/03)
A novel 3'-desphenyl-3'-cyclopropyl analogue of docetaxel was synthesized from 10-deacetyl-baccatin III. The cytotoxicity of the new taxoid was evaluated 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 that of docetaxel. This taxoid was converted to its water-soluble prodrugs that have 2'-substituted amino acid derivatives with spacer. The prodrugs had good solubility in saline and showed more potent antitumor activity against B 16 melanoma in mice than that of docetaxel.
Baccatin derivatives and processes for preparing the same
-
, (2008/06/13)
A compound represented by the formula [I]: STR1 wherein R3 represents a lower alkanoyl group; R4 represents a substituted or unsubstituted benzoyl group; ring A represents a substituted or unsubstituted cyclopropane ring; X represent