Epi-xanthatin의 Side Chain 변환을 통한 새로운 반합성 유도체들의 합성 및 세포독성

• 영문명: Synthesis of New Semisynthetic Analogs of Epi-xanthatin by Modification of the Side Chain and Their Cytotoxic Activity
• 발행기관: 대한약학회
• 저자명: 백두종(Du-Jong Bae) 안종웅(Jong-Woong Ahn) 이정옥(Chongock Lee)
• 간행물 정보: 『약학회지』제49권 제1호 (2005년), 68~73쪽, 전체 6쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2005.02.28

영문 초록

Epi-xanthatin analogs containing hydrophilic substituents such as carboxylic acid, alcohol, morpholine, amino acid, and glucose derivatives were synthesized and their in vitro cytotoxicity and in vitro antitumor activity were evaluated. The target compounds were generally cytotoxic against tumor cell lines of human origin with ED so values of 0.1-30㎍/ml, except the highly hydrophilic analog 6 containing aspartic acid. Contrary to the potent cytotoxicity, weakly hydrophilic analogs 2 and 8 were not active in vivo, or even toxic to the test animals. As a result, hydrophilic analog of epi-xanthatin did not show in vitro cytotoxicity and hydrophobic analogs did not show in vivo antitumor activity thus it is presumed that amphiphilic analogs or those with medium hydrophilicity would exhibit the antitumor potency in vivo.

키워드

epi-xanthatin analogs sesquiterpene a-methylene-y-lactone in vitro cytotoxicity in vivo antitumor activity hydrophilicity