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四氢异喹啉类似物3-表乔鲁霉素和3-表雷尼霉素G的抗肿瘤活性

Antitumor activity of tetrahydroisoquinoline analogues 3-epi-jorumycin and 3-epi-renieramycin G.

作者信息

Lane Jonathan W, Estevez Alberto, Mortara Kyle, Callan Ondine, Spencer Jeffrey R, Williams Robert M

机构信息

Department of Chemistry, Colorado State University, Fort Collins, CO 80523, USA.

出版信息

Bioorg Med Chem Lett. 2006 Jun 15;16(12):3180-3. doi: 10.1016/j.bmcl.2006.03.042. Epub 2006 May 2.

Abstract

Analogues of the tetrahydroisoquinoline family of antitumor antibiotics, 3-epi-jorumycin (3) and 3-epi-renieramycin G (4), in addition to their respective parent natural products (-)-jorumycin (1) and (-)-renieramycin G (2) were evaluated against both human colon (HCT-116) and human lung (A549) cancer cell lines. (-)-Jorumycin (1) displayed potent growth inhibition with GI50 values in the low nanomolar range (1.9-24.3 nM), while compounds 2-4 were found to be substantially less cytotoxic (GI50 0.6-14.0 microM).

摘要

对四氢异喹啉类抗肿瘤抗生素的类似物3-表-约鲁霉素(3)和3-表-雷尼霉素G(4),以及它们各自的母体天然产物(-)-约鲁霉素(1)和(-)-雷尼霉素G(2),针对人结肠(HCT-116)和人肺(A549)癌细胞系进行了评估。(-)-约鲁霉素(1)表现出强效的生长抑制作用,其GI50值在低纳摩尔范围内(1.9 - 24.3 nM),而化合物2 - 4的细胞毒性则显著较低(GI50为0.6 - 14.0 microM)。

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