1,2-dithiolan-3-ones and derivatives structurally related to leinamycin. Synthesis and biological evaluation

Farmaco. 2003 Sep;58(9):995-8. doi: 10.1016/S0014-827X(03)00134-4.

Abstract

Leinamycin, an antitumor antibiotic isolated from Streptomyces sp., shows a 1,2-dithiolan-3-one 1-oxide heterocycle that appears to be involved in the biological activity. Several derivatives related to 1,2-dithiolan-3-one 1-oxide have been prepared and their activity as antineoplastic agents have been investigated. The synthesized compounds did not display a significative antitumor or cytotoxic activity in vitro.

Publication types

  • Comparative Study

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Heterocyclic Compounds, 2-Ring / chemical synthesis
  • Heterocyclic Compounds, 2-Ring / chemistry*
  • Heterocyclic Compounds, 2-Ring / pharmacology
  • Humans
  • Lactams*
  • Macrolides / chemistry*
  • Sulfhydryl Compounds / chemistry*
  • Sulfhydryl Compounds / pharmacology
  • Thiazoles / chemistry*
  • Thiones / chemistry*

Substances

  • Antineoplastic Agents
  • Heterocyclic Compounds, 2-Ring
  • Lactams
  • Macrolides
  • Sulfhydryl Compounds
  • Thiazoles
  • Thiones
  • leinamycin