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Synthesis and biological evaluation of N-substituted benzo[c]phenanthrolines and benzo[c]phenanthrolinones as antiproliferative agents

Authors
Journal
European Journal of Medicinal Chemistry
0223-5234
Publisher
Elsevier
Volume
46
Issue
6
Identifiers
DOI: 10.1016/j.ejmech.2011.02.065
Keywords
  • Benzo[C]Phenanthrolines
  • Benzo[C]Phenanthrolinones
  • Dialkylaminoalkyl Side Chains
  • Cytotoxicity
  • Dna Interactions

Abstract

Graphical abstract Biological evaluation of N5-substituted benzo[c]phenanthrolines and C6-substituted benzo[c]phenanthrolinones shows interessant cytotoxicity associated with some DNA interactions. However, the low topoisomerase 1 affinity suggests that other cellular targets are involved. Highlights ► Pharmacomodulation of natural alkaloids to improve their profiles as anticancer agents. ► New generation of aza-analogues: benzo[c]phenanthrolines and benzo[c]phenanthrolinones. ► Introduction of dialkylaminoalkyl chains. ► Replacement of a benzene by a pyridine. ► Increased cytotoxicity and DNA affinity.

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