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New highly active taxoids from 9beta-dihydrobaccatin-9,10-acetals. Part 3
Authors:Takeda Yasuyuki  Yoshino Toshiharu  Uoto Kouichi  Chiba Jun  Ishiyama Takashi  Iwahana Michio  Jimbo Takeshi  Tanaka Noriko  Terasawa Hirofumi  Soga Tsunehiko
Institution:Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co., Ltd., Tokyo R&D Center, 16-13 Kita-Kasai 1-Chome, Edogawa-ku, Tokyo 134-8630, Japan.
Abstract:We synthesized novel water-soluble and orally active taxane analogues, 7-deoxy-9beta-dihydro-9,10-O-acetal taxanes. Cytotoxicities of the synthetic compounds were greater than those of paclitaxel and docetaxel, especially against resistant cancer cell lines expressing P-glycoprotein. In addition, some compounds showed potent antitumor effects against B16 melanoma BL6 in vivo by both iv and po administration.
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