Synthesis and evaluation of pyrazolignans. A new class of cytotoxic agents

Bioorg Med Chem. 1995 Sep;3(9):1203-10. doi: 10.1016/0968-0896(95)00091-t.

Abstract

A series of fused pyrazole derivatives of cyclolignans have been prepared through simple chemical routes and evaluated for their cytotoxic activities in culture cells of P-388 murine leukemia, A-549 lung carcinoma and HT-29 colon carcinoma. Despite the lack of the lactone moiety in their structures, they show IC50 values at microM levels.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / chemical synthesis*
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Drug Screening Assays, Antitumor
  • HT29 Cells / drug effects
  • Humans
  • Leukemia P388 / drug therapy
  • Lignans / chemical synthesis*
  • Lignans / chemistry
  • Lignans / pharmacology*
  • Lung Neoplasms / drug therapy
  • Magnetic Resonance Spectroscopy / methods
  • Mice
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents, Phytogenic
  • Lignans
  • Pyrazoles