title: New highly active taxoids from 9 beta-dihydrobaccatin-9,10-acetals. Part 5.
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.
authors.affiliation: Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co., Ltd, Tokyo R&D Center, 16-13 Kita-Kasai 1-Chome, Edogawa-ku, Tokyo 134-8630, Japan.
authors.forename: Yasuyuki
authors.initials: Y
authors.lastname: Takeda
authors.forename: Kouichi
authors.initials: K
authors.lastname: Uoto
authors.forename: Michio
authors.initials: M
authors.lastname: Iwahana
authors.forename: Takeshi
authors.initials: T
authors.lastname: Jimbo
authors.forename: Motoko
authors.initials: M
authors.lastname: Nagata
authors.forename: Ryo
authors.initials: R
authors.lastname: Atsumi
authors.forename: Chiho
authors.initials: C
authors.lastname: Ono
authors.forename: Noriko
authors.initials: N
authors.lastname: Tanaka
authors.forename: Hirofumi
authors.initials: H
authors.lastname: Terasawa
authors.forename: Tsunehiko
authors.initials: T
authors.lastname: Soga
mesh_terms: 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
chemical_list: D000970:Antineoplastic Agents; D043823:Taxoids