HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Fused aryl-phenazines: scaffold for the development of bioactive molecules.

Abstract
Fused aryl phenazine derivatives (benzo[a]phenazine, pyrido[a]phenazine, benzo[a]phenazine diones, tetrahydropyrido[a]phenazine (dermacozines), etc) are important heterocyclic compounds, which exhibit various pharmacological activities, prominently in cancer cell lines. These compounds significantly intercalate between DNA base pairs and inhibit the activities of topoisomerase I and II enzymes (Topo I and II). XR11576, XR5944, NC-190 and NC-182 belong to phenazine/fused aryl phenazine category and are under clinical studies. Several fused aryl phenazine dione compounds such as pyridazino[4,5-b]phenazine-5,12-diones, 6,11-dihydro-pyrido[2,3-b]phenazine-6,11-diones, 6,11-dihydrobenzo[2,3-b]phenazine-6,11-diones, tetrahydropyrido[a]phenazine, etc possessed anticancer activities on various cancer cell lines. Benzo[a]phenazine diimine and various other fused aryl phenazine compounds form coordination complex with the metal ions (Ru, Rh, Zn and Pt) that intercalate with the DNA and are used for the treatment of cancer. These molecules have influence on MDR cancer cells and serve as anticancer agents in MDR cancer cells. The structure activity relationship of the fused aryl phenazine derivatives revealed that the occurrence of four or more nitrogen atoms in the compounds has better anticancer activity than those molecules with less number of nitrogen atoms. Phenazine antibiotics derived from marine microbes are used for the treatment of microbial and worm diseases. Recent patents on these scaffolds showed that the benzo[a]phenazine derivatives have inhibitory activity on topoisomerase enzymes (Topo I and II) and that act as anticancer agents.
AuthorsN S Hari Narayana Moorthy, Vijayakumari Pratheepa, Maria J Ramos, Vitor Vasconcelos, Pedro A Fernandes
JournalCurrent drug targets (Curr Drug Targets) Vol. 15 Issue 7 Pg. 681-8 ( 2014) ISSN: 1873-5592 [Electronic] United Arab Emirates
PMID24499398 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
Chemical References
  • Intercalating Agents
  • Organometallic Compounds
  • Phenazines
  • Topoisomerase I Inhibitors
  • Topoisomerase II Inhibitors
Topics
  • Animals
  • Bacteria (metabolism)
  • Cell Line, Tumor
  • Cell Survival (drug effects)
  • Drug Design
  • Drug Resistance, Multiple (drug effects)
  • Drug Resistance, Neoplasm (drug effects)
  • Humans
  • Intercalating Agents (chemistry, isolation & purification, pharmacology)
  • Molecular Structure
  • Organometallic Compounds (chemistry, isolation & purification, pharmacology)
  • Phenazines (chemistry, isolation & purification, pharmacology)
  • Structure-Activity Relationship
  • Topoisomerase I Inhibitors (chemistry, isolation & purification, pharmacology)
  • Topoisomerase II Inhibitors (chemistry, isolation & purification, pharmacology)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: