Synthesis and cytotoxic evaluation of novel N-substituted amidino-1-hydroxybenzimidazole derivatives

ALP M., GÖKER A. H., ÖZKAN T., SUNGUROĞLU A.

ARCHIVES OF PHARMACAL RESEARCH, cilt.37, sa.5, ss.580-587, 2014 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 37 Sayı: 5
  • Basım Tarihi: 2014
  • Doi Numarası: 10.1007/s12272-013-0197-0
  • Dergi Adı: ARCHIVES OF PHARMACAL RESEARCH
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.580-587
  • Anahtar Kelimeler: 1H-benzimidazole, Amidinobenzimidazole, Cytotoxic activity, K562, HL-60, POTENT, PENTAMIDINE, AUTOPHAGY, DEATH
  • Ankara Üniversitesi Adresli: Evet

Özet

A new class of N-substituted amidino-1-hydroxybenzimidazole derivatives (15-24) were synthesized and evaluated for their in vitro cytotoxic activities against human leukemia cell lines, HL-60 and K562. The preliminary results showed that compounds 16, 20, 21 and 23 had moderate antitumor activity against HL-60 cell line. Further investigation on the mechanism of the observed cytotoxic effects demonstrated that compound 21 increased the expression of autophagic and apoptotic genes and induced apoptosis of HL-60 cells.