Synthesis, cytotoxicity and apoptosis of cyclotriphosphazene compounds as anti-cancer agents

YILDIRIM T., BİLGİN K., YENİLMEZ ÇİFTÇİ G., TANRIVERDİ EÇİK E., ŞENKUYTU E., Uludag Y., ...More

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol.52, pp.213-220, 2012 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 52
  • Publication Date: 2012
  • Doi Number: 10.1016/j.ejmech.2012.03.018
  • Journal Name: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Page Numbers: pp.213-220
  • Keywords: Cyclotriphosphazene, Spermine derivatives, Biological activity, Cytotoxic activity, Apoptosis, CONFORMATIONALLY RESTRICTED ANALOGS, ANTIBIOTIC SUSCEPTIBILITY, SPERMINE, POLYAMINES, GROWTH, CYCLOPHOSPHAZENES, POLYPHOSPHAZENE, DERIVATIVES, BINDING
  • Ondokuz Mayıs University Affiliated: Yes

Abstract

In the present study, a number of new dispirobino and dispiroansa spermine derivatives of cyclotriphosphazene (8-10, 13) were synthesized and characterized by elemental analysis, mass spectrometry, H-1 and P-31 NMR spectroscopy. At first, in vitro cytotoxic activity of cyclotriphosphazene compounds (1-14) against HT-29 (human colon adenocarcinoma), Hep2 (Human epidermoid larynx carcinoma), and Vero (African green monkey kidney) cell lines was investigated. Our study showed that most of these compounds stimulate apoptosis and they have cytotoxic effects for HT-29 and Hep2 cells. Additionally, these compounds (1-14) were investigated for their antibacterial activity against gram-positive (Staphylococcus aureus), gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacteria and for their antifungal activity against Candida albicans, and were shown to be inactive. (C) 2012 Elsevier Masson SAS. All rights reserved.