Synthesis and Biological Evaluation of a Novel Pyrazolecarbothioamide Derivative (DK115) Inducing Cell Cycle Arrest at the G1 Phase in HCT116 Human Colon Cancer Cells
Synthesis and Biological Evaluation of a Novel Pyrazolecarbothioamide Derivative (DK115) Inducing Cell Cycle Arrest at the G1 Phase in HCT116 Human Colon Cancer Cells
이종민(건국대학교); 신순영(건국대학교); 이영한(건국대학교); 윤혁(건국대학교); 이유리(건국대학교); 고동수(동덕여자대학교); Mi So Lee(Konkuk University)
56권 3호, 343~347쪽
초록
A novel compound, 5-(2,3-dimethoxyphenyl)-3-(1-hydroxynaphthalen-2-yl)-N-(4-methoxyphenyl)-4,5-dihydro-1Hpyrazole-1-carbothioamide (designated DK115) was synthesized,and its antitumor efficacy was assessed. Exposure of DK115 to HCT116 human colon cancer cells inhibited cellular proliferation and clonogenicity. DK115 induced cell cycle arrest at the G1phase. DK115 downregulated cyclin D1 expression, whereas upregulated p53 and p21 expressions. DK115-induced p21 was not observed in HCT116 cells lacking the p53 gene (p53–/–),suggesting that DK115 induces p21 expression via p53. These data demonstrate that a novel synthetic DK115 compound may possess antitumor activity through the induction of tumor suppressor p53-mediated G1 cell cycle arrest.
Abstract
A novel compound, 5-(2,3-dimethoxyphenyl)-3-(1-hydroxynaphthalen-2-yl)-N-(4-methoxyphenyl)-4,5-dihydro-1Hpyrazole-1-carbothioamide (designated DK115) was synthesized,and its antitumor efficacy was assessed. Exposure of DK115 to HCT116 human colon cancer cells inhibited cellular proliferation and clonogenicity. DK115 induced cell cycle arrest at the G1phase. DK115 downregulated cyclin D1 expression, whereas upregulated p53 and p21 expressions. DK115-induced p21 was not observed in HCT116 cells lacking the p53 gene (p53–/–),suggesting that DK115 induces p21 expression via p53. These data demonstrate that a novel synthetic DK115 compound may possess antitumor activity through the induction of tumor suppressor p53-mediated G1 cell cycle arrest.
- 발행기관:
- 한국응용생명화학회
- 분류:
- 농화학