New highly active taxoids from 9 beta-dihydrobaccatin-9,10-acetals. Part 5.
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.
Takeda
Yasuyuki
Y
Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co., Ltd, Tokyo R&D Center, 16-13 Kita-Kasai 1-Chome, Edogawa-ku, Tokyo 134-8630, Japan.
Uoto
Kouichi
K
Iwahana
Michio
M
Jimbo
Takeshi
T
Nagata
Motoko
M
Atsumi
Ryo
R
Ono
Chiho
C
Tanaka
Noriko
N
Terasawa
Hirofumi
H
Soga
Tsunehiko
T
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000378:metabolism / Q000627:therapeutic use; D006801:Humans; D008546:Melanoma, Experimental / Q000188:drug therapy / Q000378:metabolism; D051379:Mice; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D043823:Taxoids / Q000737:chemistry* / Q000378:metabolism / Q000627:therapeutic use
D000970:Antineoplastic Agents; D043823:Taxoids