178248-38-9Relevant academic research and scientific papers
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.
Synthesis of taxoids II. Synthesis and antitumor activity of water-soluble taxoids
Harada, Naoyuki,Ozaki, Kunihiko,Yamaguchi, Tetsuo,Arakawa, Hiroaki,Ando, Akira,Oda, Kouji,Nakanishi, Noriyuki,Ohashi, Motoaki,Hashiyama, Tomiki,Tsujihara, Kenji
, p. 241 - 258 (2007/10/03)
Synthesis of novel taxoid water-soluble prodrugs that have 2′-substituted amino acid derivatives with spacer is described. Enantioselective synthesis of the C-13 side chains proceeded through the asymmetric dihydroxylation. Several compounds had good solubility in saline and showed potent antitumor activity against B16 melanoma in mice.
