通过 X 射线衍射分析和 NMR 研究确定微管蛋白抑制剂 taltobulin（HTI-286）和 HTI-042 的绝对构型。
Absolute configurations of tubulin inhibitors taltobulin (HTI-286) and HTI-042 characterized by X-ray diffraction analysis and NMR studies.
机构信息
Wyeth Research, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1535-8. doi: 10.1016/j.bmcl.2010.01.047. Epub 2010 Jan 20.
PMID:20137930
Abstract
The stereochemistry of the tubulin inhibitors taltobulin HTI-286 (2) and HTI-042 (3) was determined by utilizing the DPFGSE 1D NOE experiment. Single crystal X-ray diffraction analysis further confirmed the absolute configuration of these two compounds, which carry the (S,S,S)-configuration necessary for biological activity.
摘要
利用 DPFGSE 1D NOE 实验确定了微管蛋白抑制剂 taltobulin HTI-286（2）和 HTI-042（3）的立体化学。单晶 X 射线衍射分析进一步证实了这两种化合物的绝对构型，它们具有生物活性所必需的（S,S,S）-构型。
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