CONJUGATE COMPOUND OF TEMOZOLOMIDE AND 5-NITRO-2(3-PHENYLPROPYLAMINO)-BENZOICACID, AND PHARMACEUTICAL COMPOSITION FOR PREVENTION AND TREATMENT OF CANCER COMPRISING THE COMPOUND
한국과학기술연구원;KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
发明人:
CHOI, KEE HYUN,최기현,YOON, HO JONG,윤호종,PARK, MI RI,박미리,JU, HEE YOUNG,주희영,PARK, SHUL KI,박슬기,CHOI, KEE HYUNKR,YOON, HO JONGKR,PARK, MI RIKR,JU, HEE YOUNGKR,PARK, SHUL KIKR
申请号：
KR1020140149827
公开号：
KR1020160052012A
申请日:
2014.10.31
申请国别(地区):
KR
年份:
2016
代理人:
摘要：
The present invention relates to a conjugate compound of temozolomide (TMZ) as a brain tumor treating agent with 5-nitro-2-(3-phenylpropylamino)benzoic acid (NPPB) as a chloride channel inhibitor (hereinafter, TMZ-NPPB), or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The compound according to the present invention has activity of cancer cell apoptosis and activity of inhibiting cancer cell invasion at the same time, and thus shows excellent anti-cancer activity. Therefore, the compound can be useful for preventing and treating various types of cancers, such as malignant glioblastoma, melanoma, glioblastoma, brain cancer, esophageal cancer, pancreatic cancer, lung cancer, invasive rectal cancer, breast cancer, metastatic prostatic cancer, ovarian cancer, or the like.본 발명은 뇌종양 치료제인 테모졸로마이드(temozolomide, TMZ)를 클로라이드 채널 저해제인 5-니트로-2-(3-페닐프로필아미노)벤조산 (5-nitro-2(3-phenylpropylamino)-benzoic acid, NPPB)를 결합한 화합물(이하, TMZ-NPPB로 약칭한다.) 또는 이의 약제학적으로 허용 가능한 염, 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학 조성물에 관한 것이다.본 발명에 따른 화합물은 암 세포에 대한 세포사멸 활성과 세포침습 저해활성을 동시에 가짐으로써 뛰어난 항암활성을 나타내는바, 악성 신경교아종, 흑색종, 아교모세포종 및 기타 뇌암, 식도암, 췌장암, 폐암, 침윤성 직장암, 유방암, 전이성 전립선암, 난소암 등과 같은 다양한 암의 예방 및 치료에 유용하게 사용될 수 있다.
