Synthesis and biological evaluation of 1,5-naphthyridines as topoisomerase I inhibitors. A new family of antiproliferative agents

Curr Top Med Chem. 2014;14(23):2722-8. doi: 10.2174/1568026614666141215152441.

Abstract

The synthesis of a variety of phenyl- and indeno-1,5-naphthyridine derivatives as new substrates with anticancer activity is described. Several of the prepared products were addressed to in vitro anticancer screening which indicated that some of them exhibited inhibitory effect of Top1 and antiproliferative activity against human colon cancer cells (COLO 205).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Camptothecin / chemistry
  • Camptothecin / pharmacology
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • DNA Topoisomerases, Type I / chemistry*
  • High-Throughput Screening Assays
  • Humans
  • Inhibitory Concentration 50
  • Naphthyridines / chemical synthesis*
  • Naphthyridines / chemistry
  • Naphthyridines / pharmacology
  • Structure-Activity Relationship
  • Topoisomerase I Inhibitors / chemical synthesis*
  • Topoisomerase I Inhibitors / chemistry
  • Topoisomerase I Inhibitors / pharmacology

Substances

  • Antineoplastic Agents
  • Naphthyridines
  • Topoisomerase I Inhibitors
  • DNA Topoisomerases, Type I
  • TOP1 protein, human
  • Camptothecin