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Synthesis and cytotoxic evaluation of novel N-substituted amidino-1-hydroxybenzimidazole derivatives
Alp, Mehmet,Goker, Hakan,Ozkan, Tulin,Sunguroglu, Asuman 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.5
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.
Synthesis and cytotoxic evaluation of novel N-substituted amidino-1-hydroxybenzimidazole derivatives
Mehmet Alp,Hakan Go¨ker,Tulin Ozkan,Asuman Sunguroglu 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.5
A new class of N-substituted amidino-1-hydroxybenzimidazole derivatives (15–24) were synthesizedand evaluated for their in vitro cytotoxic activitiesagainst human leukemia cell lines, HL-60 and K562. Thepreliminary results showed that compounds 16, 20, 21 and23 had moderate antitumor activity against HL-60 cell line. Further investigation on the mechanism of the observedcytotoxic effects demonstrated that compound 21 increasedthe expression of autophagic and apoptotic genes andinduced apoptosis of HL-60 cells.
A. Selen Gurkan-Alp,Hakan Go¨ker,Mehmet Alp,Tulin Ozkan,Asuman Sunguroglu 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.5
A series of novel 2-(4-phenoxyphenyl)-1Hbenzimidazolederivatives was synthesized and testedin vitro on human chronic myelogenous leukemia (CML)cell line K562. Benzimidazoles containing 5-amidino (10),5-N-isopropylamidino (11), 5-bromo (13), and 5,6-dimethyl(14) derivatives exhibited remarkable cytotoxicactivity. The quantitative analysis of apoptosis by flowcytometrydemonstrated that the percentages of early andlate apoptotic K562 cells treated with these compoundswere significantly higher than cells without treatment. Wealso investigated the effects of these compounds on theexpression of apoptosis-related genes BAX, BCL-2, BADand BIM. Treatment of K562 cells wih compounds 10–14significantly increased the expression levels of the proapoptoticgenes BAX, BAD and BIM, whereas compound20 increased BAX and BAD.