1-beta-D-Arabinofuranosylcytosine-5''-methylthioacetate의 합성 및 이의 DNA 합성에 대한 억제작용 평가

• 영문명: Synthesis of 1-beta-D-Arabinofuranosylcytosine-5''-methylthioacetate and Evaluation of Its Inhibitory Effect on DNA Synthesis
• 발행기관: 대한약학회
• 저자명: 이희주(Hee Joo Lee) 송민경(Min Kyung H.Song)
• 간행물 정보: 『약학회지』제30권 제5호 (1986년), 238~244쪽, 전체 7쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1986.10.30

영문 초록

As one of the starting materials, methylthioacetyl chloride(7) was synthesized in fair yield from mercaptoacetic acid via methyl methylthioacetate(5) prepared by alkylation employing N,N''-dicyclohexyl-0-methylisourea(4). Then 1-beta-D-arabinofuranosylcytosine-5'-methylthioacetate(3) was prepared by esterification of ara-C with obtained methylthioacetyl chloride and tested for inhibitory activity on DNA synthesis in the growing primary hepatocytes and hepatoma strains(H4-II-E and HTC cells). In these in vitro cell lines, the inhibitory effect of ara-C-MTA(3) on DNA synthesis was similar to that of its parent ara-C but slightly lower.