New taxanes as highly efficient reversal agents for multidrug resistance in cancer cells

Bioorg Med Chem Lett. 1998 Jan 20;8(2):189-94. doi: 10.1016/s0960-894x(97)10218-9.

Abstract

New non-cytotoxic taxanes synthesized from 10-deacetylbaccatin III and special hydrophobic acylating agents show remarkable MDR reversal activity (< or = 99.8%) against drug-resistant human breast cancer cells when co-administered with paclitaxel or doxorubicin. This activity is ascribed to the highly efficient blocking of P-glycoprotein efflux by these new taxanes.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • Animals
  • Dose-Response Relationship, Drug
  • Drug Resistance, Multiple*
  • Humans
  • Structure-Activity Relationship
  • Taxoids*
  • Triterpenes / chemistry*
  • Triterpenes / pharmacology
  • Tumor Cells, Cultured

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Taxoids
  • Triterpenes
  • 10-deacetylbaccatine III