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

Yildirim T., Bilgin K., Çiftçi G. Y., Eçik E., Şenkuytu E., Uludaǧ Y., ...Daha Fazla

European Journal of Medicinal Chemistry, cilt.52, ss.213-220, 2012 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 52
  • Basım Tarihi: 2012
  • Doi Numarası: 10.1016/j.ejmech.2012.03.018
  • Dergi Adı: European Journal of Medicinal Chemistry
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.213-220
  • Anahtar Kelimeler: Cyclotriphosphazene, Spermine derivatives, Biological activity, Cytotoxic activity, Apoptosis, CONFORMATIONALLY RESTRICTED ANALOGS, ANTIBIOTIC SUSCEPTIBILITY, SPERMINE, POLYAMINES, GROWTH, CYCLOPHOSPHAZENES, POLYPHOSPHAZENE, DERIVATIVES, BINDING
  • Atatürk Üniversitesi Adresli: Hayır

Özet

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.