A NOVEL PYRIDO-THIENO-PYRIMIDINE DERIVATIVE ACTIVATES P53 THROUGH INDUCTION OF PHOSPHORYLATION AND ACETYLATION IN COLORECTAL CANCER CELLS, AND PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF CANCER COMPRISING IT
KOREA INSTITUTE OF RADIOLOGICAL & MEDICAL SCIENCES;한국원자력의학원
发明人:
JEONG, JAE HOON,정재훈,KANG, MI AE,강미애,KIM, MI SOOK,김미숙,SONG, JIE YOUNG,송지영,JEONG, JAE HOONKR,KANG, MI AEKR,KIM, MI SOOKKR,SONG, JIE YOUNGKR
申请号:
KR1020150015944
公开号:
KR1020160094673A
申请日:
2015.02.02
申请国别(地区):
KR
年份:
2016
代理人:
摘要:
The present invention relates to a composition for promoting activities of p53 comprising N-[2-(dimethylamino)ethyl]-2,3-dimethyl-4-oxo-4H-pyrido[1,2-a]thieno[2,3-d]pyrimidine-9-carboxamide (PTP), which is a pyrido-thieno-pyrimidine derivative and represented by chemical formula 1, or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical uses of the composition. The derivative induces expression and activation of p53, which is a tumor inhibitory protein, in tumor cells, thereby showing apoptosis and growth inhibition effects of tumor cells.본 발명은 Pyrido-thieno-pyrimidine 유도체인 N-[2-(dimethylamino)ethyl]-2,3-dimethyl-4-oxo-4H-pyrido[1,2-a]thieno[2,3-d]pyrimidine-9-carboxamide (PTP) 또는 그의 약제학적으로 허용 가능한 염을 포함하는 p53 활성 증진용 조성물 및 그의 약학적 용도에 관한 것이다.상기 유도체는 종양 세포에서 종양억제 단백질인 p53의 발현과 활성화를 유도하며, 그에 따라 종양 세포의 사멸과 생장 억제 작용을 나타낸다.