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New highly active taxoids from 9 beta-dihydrobaccatin-9,10-acetals. Part 5
Yasuyuki Takeda1, Kouichi Uoto, Michio Iwahana
1Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co., Ltd, Tokyo R&D Center, 16-13 Kita-Kasai 1-Chome, Edogawa-ku, Tokyo 134-8630, Japan.
Bioorganic & Medicinal Chemistry Letters
|May 20, 2004
Abstract:
To improve the metabolic stability of 3, which exhibited both in vitro antitumor activity and in vivo efficacy by both iv and po administration, we designed and synthesized new taxane analogues. Most of the synthetic compounds maintained excellent antitumor activity and were scarcely metabolized by human liver microsomes. And some compounds exhibited potent antitumor effects against B16 melanoma BL6 in vivo by both iv and po administration similarly to 3.