New highly active taxoids from 9beta-dihydrobaccatin-9,10-acetals. Part 3

  • Bioorg Med Chem Lett. 2003 Jan 20;13(2):185-90. doi: 10.1016/s0960-894x(02)00891-0.
Yasuyuki Takeda  1 ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Jun Chiba ,  Takashi Ishiyama ,  Michio Iwahana ,  Takeshi Jimbo ,  Noriko Tanaka ,  Hirofumi Terasawa ,  Tsunehiko Soga
Affiliations
  • 1. Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co., Ltd., Tokyo R&D Center, 16-13 Kita-Kasai 1-Chome, Edogawa-ku, Tokyo 134-8630, Japan.
PMID: 12482420 DOI: 10.1016/s0960-894x(02)00891-0
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.