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KMID : 0043320140370050580
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Archives of Pharmacal Research
2014 Volume.37 No. 5 p.580 ~ p.587
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Synthesis and cytotoxic evaluation of novel N-substituted amidino-1-hydroxybenzimidazole derivatives
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Alp Mehmet
Goker Hakan
Ozkan Tulin
Sunguroglu Asuman
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Abstract
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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.
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KEYWORD
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1H-benzimidazole, Amidinobenzimidazole, Cytotoxic activity, K562, HL-60
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