Design, synthesis and biological activity of novel C2-C3' N-Linked macrocyclic taxoids

Bioorg Med Chem Lett. 2002 Feb 11;12(3):349-52. doi: 10.1016/s0960-894x(01)00747-8.

Abstract

A series of novel macrocyclic taxoids was designed and synthesized by connecting the C-2 and C-3' N positions of the taxoid framework with various tethers. Cytotoxicity of these macrocyclic taxoids was evaluated against a human breast cancer cell line LCC6-WT, and a couple of the taxoids exhibited 0.09-0.3 microM IC(50) values.

Publication types

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

MeSH terms

  • Antineoplastic Agents, Phytogenic / chemical synthesis*
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Breast Neoplasms / drug therapy
  • Cell Survival / drug effects
  • Crystallography, X-Ray
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Female
  • Humans
  • Indicators and Reagents
  • Molecular Conformation
  • Paclitaxel / analogs & derivatives*
  • Paclitaxel / chemical synthesis
  • Paclitaxel / pharmacology
  • Stereoisomerism
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents, Phytogenic
  • Indicators and Reagents
  • Paclitaxel