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从红藻霍氏波蒂藻中分离出的与卤代单萜相关的抗肿瘤单萜及其结构/活性特征

Isolation and structure/activity features of halomon-related antitumor monoterpenes from the red alga Portieria hornemannii.

作者信息

Fuller R W, Cardellina J H, Jurek J, Scheuer P J, Alvarado-Lindner B, McGuire M, Gray G N, Steiner J R, Clardy J, Menez E

机构信息

Laboratory of Drug Discovery Research and Development, National Cancer Institute, Frederick, Maryland 21702-1201.

出版信息

J Med Chem. 1994 Dec 9;37(25):4407-11. doi: 10.1021/jm00051a019.

DOI:10.1021/jm00051a019
PMID:7996553
Abstract

Ten halogenated monoterpenes (2-6 and 8-12) related to the novel antitumor compound halomon (1) or to the carbocyclic analog 7 have been isolated from different geographic collections of the red alga, Portieria hornemannii. Structures were assigned to the basis of spectral analyses (primarily NMR and MS). The absolute configuration of isohalomon (2) was further established by X-ray crystallography. The compounds were comparatively evaluated alongside 1 and 7 in the U.S. National Cancer Institute's in vitro human tumor cell line screening panel. The results provide some interesting initial insights into the structure/activity relationships in this series.

摘要

从红藻角叉菜不同地理区域的样本中分离出了10种与新型抗肿瘤化合物卤代霉素(1)或碳环类似物7相关的卤代单萜(2 - 6和8 - 12)。通过光谱分析(主要是核磁共振和质谱)确定了它们的结构。异卤代霉素(2)的绝对构型通过X射线晶体学进一步确定。在美国国立癌症研究所的体外人类肿瘤细胞系筛选小组中,将这些化合物与1和7进行了比较评估。结果为该系列化合物的结构/活性关系提供了一些有趣的初步见解。

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