Studies directed towards the refinement of the pancratistatin cytotoxic pharmacophore

Bioorg Med Chem Lett. 2001 Jan 22;11(2):169-72. doi: 10.1016/s0960-894x(00)00614-4.

Abstract

Two deoxy-analogues of the anticancer/antiviral agent pancratistatin containing functionality complementary to the minimum structural pharmacophore were synthesized and subjected to anticancer screening. One of the analogues exhibited selective inhibition of certain tumor cell lines but was significantly less potent than the natural products. The minimum structural pharmacophore has now been refined from eight to three possible structures.

Publication types

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

MeSH terms

  • Amaryllidaceae Alkaloids*
  • Animals
  • Antineoplastic Agents, Phytogenic / chemical synthesis*
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / pharmacology
  • Cell Division / drug effects
  • Drug Screening Assays, Antitumor
  • Humans
  • Inhibitory Concentration 50
  • Isoquinolines / chemical synthesis
  • Isoquinolines / chemistry
  • Isoquinolines / pharmacology*
  • Mice
  • Models, Molecular
  • Structure-Activity Relationship
  • Tumor Cells, Cultured / drug effects

Substances

  • Amaryllidaceae Alkaloids
  • Antineoplastic Agents, Phytogenic
  • Isoquinolines
  • pancratistatin