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

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3209-15. doi: 10.1016/j.bmcl.2004.03.109.

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.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / therapeutic use
  • Humans
  • Melanoma, Experimental / drug therapy
  • Melanoma, Experimental / metabolism
  • Mice
  • Microsomes, Liver / drug effects
  • Microsomes, Liver / metabolism
  • Taxoids / chemistry*
  • Taxoids / metabolism
  • Taxoids / therapeutic use

Substances

  • Antineoplastic Agents
  • Taxoids