新型吲哚基-1,3,4-恶二唑作为强效抗癌剂的高效合成及生物学研究
An efficient synthesis and biological study of novel indolyl-1,3,4-oxadiazoles as potent anticancer agents.
作者信息
Kumar Dalip, Sundaree Swapna, Johnson Emmanuel O, Shah Kavita
机构信息
Chemistry Group, Birla Institute of Technology and Science, Pilani 333 031, India.
出版信息
Bioorg Med Chem Lett. 2009 Aug 1;19(15):4492-4. doi: 10.1016/j.bmcl.2009.03.172. Epub 2009 Jun 13.
A facile, convenient and high yielding synthesis of a series of novel 5-(3'-indolyl)-2-(substituted)-1,3,4-oxadiazoles from readily available starting materials has been described. The key step of this protocol is oxidative cyclization of N-acylhydrazones 1 using [bis(trifluoroacetoxy)iodo]benzene under solvent-free condition. The 5-(3'-indolyl)-2-(substituted)-1,3,4-oxadiazoles were screened for their in vitro anticancer activity against various human cancer cell lines. Compounds 3c, 3d and 3j exhibited potent cytotoxicity (IC(50) approximately 1microM) and selectivity against human cancer cell lines.
已经描述了一种从容易获得的起始原料出发，简便、便捷且高产率地合成一系列新型5-(3'-吲哚基)-2-(取代)-1,3,4-恶二唑的方法。该方案的关键步骤是在无溶剂条件下使用[双(三氟乙酰氧基)碘]苯对N-酰基腙1进行氧化环化。对5-(3'-吲哚基)-2-(取代)-1,3,4-恶二唑针对各种人类癌细胞系的体外抗癌活性进行了筛选。化合物3c、3d和3j表现出强大的细胞毒性（IC(50)约为1微摩尔）以及对人类癌细胞系的选择性。
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