Bioorganic & Medicinal Chemistry Letters 2004-06-21

New highly active taxoids from 9 beta-dihydrobaccatin-9,10-acetals. Part 5.

Yasuyuki Takeda, Kouichi Uoto, Michio Iwahana, Takeshi Jimbo, Motoko Nagata, Ryo Atsumi, Chiho Ono, Noriko Tanaka, Hirofumi Terasawa, Tsunehiko Soga

Index: Bioorg. Med. Chem. Lett. 14(12) , 3209-3215, (2004)

Full Text: HTML

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.