乙酰基-4H,9H-萘并[2,3-b]噻吩-4,9-二酮的合成与细胞毒性

Synthesis and cytotoxicity of acetyl-4H,9H-naphtho[2,3-b]thiophene-4,9-diones.

作者信息

Huang L J, Kuo S C, Perng C Y, Chao Y H, Wu T S, McPhail A T, Mauger A, Cheng H H, Lee K H

机构信息

Graduate Institute of Pharmaceutical Chemistry, China Medical College, Taichung, Taiwan, Republic of China.

出版信息

Bioorg Med Chem Lett. 1998 Oct 6;8(19):2763-8. doi: 10.1016/s0960-894x(98)00496-x.

DOI:10.1016/s0960-894x(98)00496-x

PMID:9873618

Abstract

Several new acetyl-4H,9H-naphtho[2,3-b]thiophene-4,9-diones were synthesized and evaluated for in vitro cytotoxicity by NCI against seven cancer cell types. 2,7-Diacetyl naphtho[2,3-b]thiophene-4,9-dione (9) showed significant cytotoxicity against leukemia cells with log GI50 values of -7.61 against SR cells and -7.18 against MOLT-4 cells. 3-Acetyl-naphtho[2,3-b]thiophene-4,9-dione (6) also demonstrated potent cytotoxicity in the latter cell line with log GI50 < -8.

摘要

合成了几种新型的乙酰基-4H,9H-萘并[2,3-b]噻吩-4,9-二酮，并由美国国立癌症研究所（NCI）评估了它们对七种癌细胞系的体外细胞毒性。2,7-二乙酰基萘并[2,3-b]噻吩-4,9-二酮（9）对白血病细胞显示出显著的细胞毒性，对SR细胞的对数GI50值为-7.61，对MOLT-4细胞的对数GI50值为-7.18。3-乙酰基-萘并[2,3-b]噻吩-4,9-二酮（6）在后一种细胞系中也表现出强效细胞毒性，对数GI50 < -8。