1-甲苯磺酰基-3-[(3'-羟基-5'-取代的)-γ-丁内酯]-吲哚：合成、COX-2抑制作用及抗癌活性
1-Toluene-sulfonyl-3-[(3'-hydroxy-5'-substituted)-gamma-butyrolactone]-indoles: synthesis, COX-2 inhibition and anti-cancer activities.
作者信息
Singh Palwinder, Mittal Anu, Bhardwaj Atul, Kaur Satwinderjeet, Kumar Subodh
机构信息
Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
出版信息
Bioorg Med Chem Lett. 2008 Jan 1;18(1):85-9. doi: 10.1016/j.bmcl.2007.11.010. Epub 2007 Nov 6.
Indoles carrying a cyclic ester (gamma-butyrolactone) at C-3 position have been synthesized by the allylation of 3-indoleglyoxylate followed by iodocyclisation and the nucleophilic replacement of the iodo-group. Screening of these molecules for COX-2 inhibition and anti-cancer activities has identified compounds 10 and 11 as highly potent and selective for COX-2 as well as showing remarkable anti-cancer activities (better than that of indomethacin).
通过3-吲哚乙醛酸酯的烯丙基化反应，随后进行碘环化反应以及碘基团的亲核取代反应，合成了在C-3位带有环状酯（γ-丁内酯）的吲哚类化合物。对这些分子进行COX-2抑制和抗癌活性筛选，已鉴定出化合物10和11对COX-2具有高效和选择性，并且显示出显著的抗癌活性（优于吲哚美辛）。
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