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.

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.

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / chemical synthesis*
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / pharmacology
  • Cell Survival / drug effects
  • Crystallography, X-Ray
  • Drug Screening Assays, Antitumor
  • Humans
  • Indicators and Reagents
  • Melanoma, Experimental / drug therapy
  • Mice
  • Molecular Conformation
  • Neoplasm Transplantation
  • Paclitaxel / analogs & derivatives*
  • Paclitaxel / chemical synthesis*
  • Paclitaxel / pharmacology
  • Solubility
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents, Phytogenic
  • Indicators and Reagents
  • Paclitaxel