A novel anti-tumor agent, Ln(III) 2-thioacetate benzothiazole induces anti-angiogenic effect and cell death in cancer cell lines.

Abstract

New complexes with a potent DNA-binding anti-tumor agent, europium(III)- and terbium(III)-2-thioacetate benzothiazole were synthesized and characterized. These complexes showed strong binding affinity to calf thymus DNA using fluorometric and electronic absorption spectroscopy. The synthesized complexes resulted in inhibition of proliferation of EAC cells and ascites formation. Their anti-tumor effect was found to be through anti-angiogenic activity as was evident by the reduction of microvessel density and down-regulation of VEGF receptor type-2 (Flk-1). It was found that EAC cells had distinct DNA fragmentation patterns analyzed by capillary electrophoresis in the treated animals. Moreover, the synthesized complexes exhibited significant cytotoxic activity against HepG2 and MCF7 cell lines. Furthermore, complexes showed a potent anti-bacterial activity against two pathogenic bacteria Escherichia coli and Salmonella.

• Authors: Belal H M Hussein, Hassan A Azab, Mona F el-Azab, Abdullah I el-Falouji
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 51 Pg. 99-109 (May 2012) ISSN: 1768-3254 [Electronic] France
• PMID: 22424613 (Publication Type: Journal Article)
• Copyright: Copyright © 2012 Elsevier Masson SAS. All rights reserved.

Chemical References

• Angiogenesis Inhibitors
• Anti-Bacterial Agents
• Antineoplastic Agents
• Benzothiazoles
• Organometallic Compounds
• Terbium
• Europium
• DNA
• calf thymus DNA
• benzothiazole

Topics

• Angiogenesis Inhibitors (chemistry, metabolism, pharmacology, therapeutic use)
• Animals
• Anti-Bacterial Agents (chemistry, metabolism, pharmacology, therapeutic use)
• Antineoplastic Agents (chemistry, metabolism, pharmacology, therapeutic use)
• Benzothiazoles (chemistry)
• Carcinoma, Ehrlich Tumor (blood supply, pathology)
• Cell Death (drug effects)
• Cell Line, Tumor
• DNA (metabolism)
• DNA Fragmentation (drug effects)
• Escherichia coli (drug effects)
• Europium (chemistry)
• Female
• Humans
• Mice
• Neovascularization, Pathologic (drug therapy)
• Organometallic Compounds (chemistry, metabolism, pharmacology, therapeutic use)
• Salmonella (drug effects)
• Terbium (chemistry)
• Tumor Burden (drug effects)