Magedov Igor V, Luchetti Giovanni, Evdokimov Nikolai M, Manpadi Madhuri, Steelant Wim F A, Van Slambrouck Severine, Tongwa Paul, Antipin Mikhail Yu, Kornienko Alexander
Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, USA.
Bioorg Med Chem Lett. 2008 Feb 15;18(4):1392-6. doi: 10.1016/j.bmcl.2008.01.019. Epub 2008 Jan 11.
Diversely substituted 2-pyrrolines have been prepared by a novel multicomponent process involving a reaction of various N-(aryl- and alkylsulfonamido)-acetophenones with aldehydes and malononitrile. While the reaction is highly regioselective, it is not stereoselective, generating a mixture of cis and trans 2-pyrrolines. A number of analogs from both cis and trans 2-pyrroline libraries were found to have antiproliferative activity in human cancer cell lines.
通过一种新型多组分过程制备了多种取代的2-吡咯啉，该过程涉及各种N-（芳基和烷基磺酰胺基）苯乙酮与醛和丙二腈的反应。虽然该反应具有高度的区域选择性，但不具有立体选择性，生成顺式和反式2-吡咯啉的混合物。发现来自顺式和反式2-吡咯啉文库的许多类似物在人癌细胞系中具有抗增殖活性。
