Synthesis and characterization of copper(II) and zinc(II)-based potential chemotherapeutic compounds: their biological evaluation viz. DNA binding profile, cleavage and antimicrobial activity.

Abstract

Metal-based cancer chemotherapeutic agents of the type [Cu(phen)TzCl(2)]H(2)O 1 and [Zn(phen)(Tz)Cl(2)·H(2)O] 2, where phen = 1,10-phenanthroline and Tz = 1,2,4-triazole have been synthesized and characterized by various spectroscopic and analytical techniques. The structure of complex 1 was also determined by X-ray crystallography. The in vitro DNA binding studies of complexes 1 and 2 with CT DNA were carried out by various biophysical and molecular docking techniques. Both the complexes cleave supercoiled pBR322 DNA via hydrolytic pathway, as validated by T4 DNA ligase assay. Furthermore, both complexes exhibited significant antimicrobial activity. The results revealed that complex 1 has better prospectus to act as cancer chemotherapeutic candidate which warrants further in vitro and in vivo anticancer investigations.

• Authors: Sartaj Tabassum, Ahmad Asim, Farukh Arjmand, Mohd Afzal, Vivek Bagchi
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 58 Pg. 308-16 (Dec 2012) ISSN: 1768-3254 [Electronic] France
• PMID: 23137447 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2012 Elsevier Masson SAS. All rights reserved.

Chemical References

• Anti-Bacterial Agents
• Antifungal Agents
• Organometallic Compounds
• Reactive Oxygen Species
• Copper
• DNA
• Zinc

Topics

• Anti-Bacterial Agents (chemical synthesis, chemistry, pharmacology)
• Antifungal Agents (chemical synthesis, chemistry, pharmacology)
• Antineoplastic Combined Chemotherapy Protocols (chemical synthesis, chemistry, pharmacology)
• Binding Sites (drug effects)
• Copper (chemistry)
• Crystallography, X-Ray
• DNA (chemistry, drug effects)
• DNA Cleavage (drug effects)
• Dose-Response Relationship, Drug
• Fungi (drug effects)
• Gram-Negative Bacteria (drug effects)
• Gram-Positive Bacteria (drug effects)
• Microbial Sensitivity Tests
• Models, Molecular
• Molecular Structure
• Organometallic Compounds (chemical synthesis, chemistry, pharmacology)
• Plasmids (chemistry, drug effects)
• Reactive Oxygen Species (metabolism)
• Structure-Activity Relationship
• Viscosity
• Zinc (chemistry)