NOVEL GELDANAMYCIN DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREOF AND AGENT FOR THE PREVENTION AND TREATMENT OF TUMOR CONTAINING THE SAME AS AN ACTIVE INGREDIENT
KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY;한국생명공학연구원
发明人:
HONG, YOUNG SOO,홍영수,WU CHENGZHU,오성주,LEE, DONG HO,이동호,LEE, JUNG JOON,이정준
申请号：
KR1020100109792
公开号：
KR1020120048249A
申请日:
2010.11.05
申请国别(地区):
KR
年份:
2012
代理人:
摘要：
PURPOSE: A novel geldanamycin derivative and a therapeutic agent containing the same are provided to suppress Hsp90 activity and Her2 and c-raf expression and to be used in cancer therapeutic agent, antibiotics, antifungal agent, antiviral agent, and anti-inflammatory agent. CONSTITUTION: A geldanamycin derivative is denoted by chemical formula 1. A method for manufacturing the derivative comprises: a step of culturing recombinant Streptomyces hygroscopicus mutant strain to prepare culture liquid； a step of extracting the culture liquid by ethyl acetate and fractioning to obtain a fraction； a step of performing silica gel chromatography of the fraction to prepare an active fraction； and a step of isolating the compound of chemical formula 1. A pharmaceutical composition for preventing and treating cancer contains the derivative or pharmaceutically acceptable salt thereof as an active ingredient.본 발명은 하기 화학식 1로 표시되는 신규한 젤다나마이신 유도체, 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 암 예방 및 치료제에 관한 것으로서, 본 발명의 상기 젤다나마이신 유도체는 ATPase 활성을 저해하고, 암세포의 성장 및 전이에 중요한 역할을 수행하는 샤페론 단백질인 Hsp90의 활성을 저해하며, Her2 및 c-raf 단백질의 발현을 저해함으로써, 암 치료제뿐만 아니라, 항생제, 항진균제, 항바이러스제, 면역억제제, 퇴행성 신경 질환 치료제, 항염증제 등으로 유용하게 사용될 수 있다. [화학식 1](상기 화학식 1에서, R은 본 명세서에서 정의된 바와 같다)
