PMID- 24499398
OWN - NLM
STAT- MEDLINE
DCOM- 20150126
LR  - 20190911
IS  - 1873-5592 (Electronic)
IS  - 1389-4501 (Linking)
VI  - 15
IP  - 7
DP  - 2014
TI  - Fused aryl-phenazines: scaffold for the development of bioactive molecules.
PG  - 681-8
AB  - 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.
FAU - Moorthy, N S Hari Narayana
AU  - Moorthy NS
FAU - Pratheepa, Vijayakumari
AU  - Pratheepa V
FAU - Ramos, Maria J
AU  - Ramos MJ
FAU - Vasconcelos, Vitor
AU  - Vasconcelos V
FAU - Fernandes, Pedro A
AU  - Fernandes PA
AD  - REQUIMTE, Departamento de Quimica e Bioquimica, Faculdade de Ciencias, 
      Universidade do Porto, s/n, Rua do Campo Alegre, 4169-007 Porto, Portugal. 
      hari.moorthy@fc.up.pt.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
PL  - United Arab Emirates
TA  - Curr Drug Targets
JT  - Current drug targets
JID - 100960531
RN  - 0 (Intercalating Agents)
RN  - 0 (Organometallic Compounds)
RN  - 0 (Phenazines)
RN  - 0 (Topoisomerase I Inhibitors)
RN  - 0 (Topoisomerase II Inhibitors)
SB  - IM
MH  - Animals
MH  - Bacteria/metabolism
MH  - Cell Line, Tumor
MH  - Cell Survival/drug effects
MH  - *Drug Design
MH  - Drug Resistance, Multiple/drug effects
MH  - Drug Resistance, Neoplasm/drug effects
MH  - Humans
MH  - Intercalating Agents/chemistry/isolation & purification/*pharmacology
MH  - Molecular Structure
MH  - Organometallic Compounds/chemistry/isolation & purification/*pharmacology
MH  - Phenazines/chemistry/isolation & purification/*pharmacology
MH  - Structure-Activity Relationship
MH  - Topoisomerase I Inhibitors/chemistry/isolation & purification/*pharmacology
MH  - Topoisomerase II Inhibitors/chemistry/isolation & purification/*pharmacology
EDAT- 2014/02/07 06:00
MHDA- 2015/01/27 06:00
CRDT- 2014/02/07 06:00
PHST- 2013/10/29 00:00 [received]
PHST- 2014/01/26 00:00 [revised]
PHST- 2014/02/04 00:00 [accepted]
PHST- 2014/02/07 06:00 [entrez]
PHST- 2014/02/07 06:00 [pubmed]
PHST- 2015/01/27 06:00 [medline]
AID - CDT-EPUB-59046 [pii]
AID - 10.2174/1389450115666140205152007 [doi]
PST - ppublish
SO  - Curr Drug Targets. 2014;15(7):681-8. doi: 10.2174/1389450115666140205152007.