alpha-halogenoacrylic derivatives of antitumor agents

Mini Rev Med Chem. 2009 Jan;9(1):81-94. doi: 10.2174/138955709787001640.

Abstract

In this review article we have reported a series of hybrid compounds characterized by the presence of a alpha-halogenocryloyl alkylating moiety of low chemical reactivity, linked to known antitumor agents or their active moieties. Among them, brostallicin (PNU-166196), was selected for clinical development and is now undergoing Phase II studies in patients with advanced or metastatic soft tissue sarcoma.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents, Alkylating / chemistry*
  • Antineoplastic Agents, Alkylating / pharmacology
  • Cell Line, Tumor
  • Distamycins / chemistry
  • Distamycins / pharmacology
  • Guanidines / chemistry
  • Guanidines / therapeutic use
  • Humans
  • Mice
  • Pyrroles / chemistry
  • Pyrroles / therapeutic use
  • Pyrroloiminoquinones / chemistry*
  • Pyrroloiminoquinones / pharmacology

Substances

  • Antineoplastic Agents, Alkylating
  • Distamycins
  • Guanidines
  • Pyrroles
  • Pyrroloiminoquinones
  • stallimycin
  • brostallicin