YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
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Anticancer Mechanisms of 3-Heptylamino-6-Allylthiopyridazine and 3-Dipentylamino-6-Allylthiopyridazine in Human Colon Carcinoma RKO Cells

RKO 대장암세포에서 3-헵틸아미노-6-알릴티오피리다진과 3-디펜틸아미노-6-알릴티오피리다진의 항암기전

  • 임현경 (덕성여자대학교 약학대학) ;
  • 권유미 (덕성여자대학교 약학대학) ;
  • 송지윤 (덕성여자대학교 약학대학) ;
  • 김경미 (덕성여자대학교 약학대학) ;
  • 김채원 (덕성여자대학교 약학대학) ;
  • 박명숙 (덕성여자대학교 약학대학) ;
  • 정주희 (덕성여자대학교 약학대학)
  • Received : 2016.01.22
  • Accepted : 2016.03.28
  • Published : 2016.06.30
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Abstract

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-${\kappa}B$. This result suggested that compound II suppressed cell proliferation. These different mechanisms of these compounds might have occurred through different steric conformation.

Keywords

References

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