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KMID : 0370220160600030101
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Yakhak Hoeji
2016 Volume.60 No. 3 p.101 ~ p.106
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Anticancer Mechanisms of 3-Heptylamino-6-Allylthiopyridazine and 3-Dipentylamino-6-Allylthiopyridazine in Human Colon Carcinoma RKO Cells
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Lim Hyun-Kyung
Kwon Yu-Mi
Song Ji-Yun
Kim Kyoung-Mee
Kim Chae-Won
Park Myung-Sook
Jung Joo-Hee
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Abstract
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Allylthiopyridazine derivatives were synthesized and evaluated for anti-proliferative activities in the previous study. In this study, selected two allylthiopyridazine derivatives (compound I, 3-heptylamino-6-allylthiopyridazine and compound II, 3-dipentylamino-6-allylthiopyridazine) were assessed for cytotoxicity and chronic proliferation in human colon carcinoma RKO cells. Two derivatives dose-dependently inhibited cell viability and proliferation. To elucidate the anticancer mechanism of two derivatives, we investigated the expression level of apoptosis-related proteins in RKO cells. Compound I induced the activation of JNK and expression of p53 and p21. On the other hand, compound II showed no change of p53 level. Interestingly, compound II inhibited the nuclear translocation of NF-κB. This result suggested that compound II suppressed cell proliferation. These different mechanisms of these compounds might have occurred through different steric conformation.
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KEYWORD
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3-heptylamino-6-allylthiopyridazine, 3-dipentylamino-6-allylthiopyridazine, anticancer effect, RKO cell
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