The present invention relates to a novel (new) tetrahydropyridinol derivative compound and a new use thereof for cancer treatment, and more specifically, to a novel tetrahydropyridinol derivative compound, a pharmaceutical composition comprising the same as an active ingredient for preventing or treating cancer, and a health functional food. The novel tetrahydropyridinol derivative compound of the present invention can inhibit the proliferation and invasion of cancer cells by a wnt/&beta-catenin signal inhibition mechanism through down-regulation of &beta-catenin expression, up-regulation of glycogen synthase kinase 3-&beta (GSK-3&beta), or up-regulation of E-cadherin expression, and also induce cell cycle arrest of cancer cells through the inhibition of CDK2 expression and the increase of p21 and p27 expression. Therefore, the novel tetrahydropyridinol derivative of the present invention can be applied to medicine, such as a pharmaceutical composition, as well as a health function food, as a material which can prevent or treat cancer, and thus is expected to have a very high value when being applied to food industries and medicinal industries. Further, since the novel tetrahydropyridinol derivative of the present invention does not show cytotoxicity to non-tumor cells instead of cancer cells, the composition of the present invention comprising the derivative as an active ingredient has an advantage of being safe even for long-term use.COPYRIGHT KIPO 2014본 발명은 신규한(새로운) 테트라하이드로피리디놀 유도체 화합물 및 이들의 암 치료의 신규 용도에 관한 것으로, 자세하게는 신규 테트라하이드로피리디놀 유도체 화합물, 이를 유효성분으로 포함하는 암 예방 또는 치료용 약제학적 조성물, 건강기능식품에 관한 것이다. 본 발명의 신규 테트라하이드로피리디놀(tetrahydropyridinol) 유도체 화합물은 베타-카테닌(β-catenin) 발현의 하향 조절, GSK-3β(glyco-gensynthase kinsase 3-β) 발현의 상향 조절 또는 이케드헤린(E-cadherin) 발현의 상향 조절을 통한 wnt/β-catenin 신호 방해 기작으로 암세포의 증식 및 침투를 억제할 수 있을 뿐만 아니라, CDK2의 발현 억제 및 p21과 p27의 발현 증대를 통한 암세포의 세포주기중지(cell cycle arrest)를 유도할 수 있다. 따라서 본 발명의 신규 테트라하이드로피리디놀 유도체는 암을 예방 또는 치료할 수 있는 물질로서 약리학적 조성물과 같은 의약품은 물론이고, 건강기능