从N-未保护的2-氧化吲哚直接合成C3-单官能化氧化吲哚及其抗利什曼原虫活性。
Direct synthesis of C3-mono-functionalized oxindoles from N-unprotected 2-oxindole and their antileishmanial activity.
作者信息
Scala Angela, Cordaro Massimiliano, Grassi Giovanni, Piperno Anna, Barberi Giuseppina, Cascio Antonio, Risitano Francesco
机构信息
Dipartimento di Scienze Chimiche, Università di Messina, V.le F.Stagno d'Alcontres 31, Messina 98166, Italy; CNR-ISMN Istituto per lo Studio dei Materiali Nanostrutturati, UOS Palermo, c/o Dip. Scienze Chimiche, Università di Messina, V.le F.Stagno d'Alcontres 31, Messina 98166, Italy.
Dipartimento di Scienze Chimiche, Università di Messina, V.le F.Stagno d'Alcontres 31, Messina 98166, Italy.
出版信息
Bioorg Med Chem. 2014 Feb 1;22(3):1063-9. doi: 10.1016/j.bmc.2013.12.039. Epub 2013 Dec 25.
A novel approach for the synthesis of unprecedented C3-mono-functionalized indolin-2-ones is reported, starting from 2-oxindole and chalcones. The reactions proceed regioselectively under mild conditions, without di- and tri-alkylated side products. The new compounds have been evaluated in vitro for their antiproliferative effects against the protozoan Leishmania infantum. Interestingly, they appear able to kill L. infantum promastigotes and amastigotes, without significant cytotoxic effects.
报道了一种从2-氧代吲哚和查耳酮出发合成前所未有的C3-单官能化吲哚啉-2-酮的新方法。该反应在温和条件下区域选择性地进行，没有二烷基化和三烷基化副产物。已对这些新化合物进行体外评估，以研究它们对原生动物婴儿利什曼原虫的抗增殖作用。有趣的是，它们似乎能够杀死婴儿利什曼原虫的前鞭毛体和无鞭毛体，且没有明显的细胞毒性作用。
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