4-카바모일옥시메틸-1-아자얀트라퀴논 유도체들의 합성 및 세포독성

• 영문명: Synthesis and Cytotoxicity of 4-Carbamoyloxymethyl-1-azaanthraquinones
• 발행기관: 대한약학회
• 저자명: 이희순(Hee Soon Lee) 이승일(Seung Il Lee) 홍승수(Seoung Soo Hong) 조정숙(Jung Sook Cho) 김영호(Young Hoon Jung)
• 간행물 정보: 『약학회지』제42권 제5호 (1998년), 507~512쪽, 전체 6쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1998.10.31

영문 초록

In the course of developing novel antitumor intercalating agents. We synthesized 4-carbamoyloxymethyl-l-azaanthraquinones 7-12, incorporating the latent alkylating functionality. These compounds were designed to explore the effect of substituent on the nitrogen of carbamate. The target compounds were prepared by hetero Diels-Alder reaction as a key step followed by functionalization of benzylic methyl to the desired substituents. Growth inhibitory studies of the azaanthraquinones were conducted in vitro against human cancer cell lines (SNU-354; liver and MCF7; breast) and human epidermoid carcinoma cells that are sensitive (KB-3-1) and multidrug-resistant (KB-V-1). The compounds were less potent than doxorubicin against sensitive cell lines. However, the most active compound 12 was not cross-resistant with doxorubicin against KB-V-1.

키워드

Intercalating agent anthracycline mitoxatrone ametantrone doxorubicin topoisomerase Ⅱ azaanthraquinone cytotoxic activity.