Verboom W, Reinhoudt D N, Lammerink B H, Orlemans E O, van Veggel F C, Lelieveld P
Laboratory of Organic Chemistry, Twente University of Technology, AE Enschede, The Netherlands.
Anticancer Drug Des. 1987 Dec;2(3):271-7.
Mitosenes of both the pyrrolo- and pyrido[1,2-a]indole type have been prepared via a modified Madelung reaction of benzeneacetonitriles ortho-substituted with gamma- and delta-lactam moieties, respectively, followed by modification of the resulting heterotricyclic compounds. Some in vitro anti-tumour activity data of these novel compounds are rearrangement of 2-(1-pyrrolidinyl)-3-vinylquinone derivatives to 5,8-dioxo-1H-pyrrolo[1,2-a]indoles.
吡咯并[1,2 - a]吲哚型和吡啶并[1,2 - a]吲哚型的有丝分裂原已通过分别用γ - 和δ - 内酰胺部分邻位取代的苯乙腈的改良Madelung反应制备,随后对所得的杂三环化合物进行修饰。这些新型化合物的一些体外抗肿瘤活性数据是2-(1 - 吡咯烷基)-3 - 乙烯基醌衍生物重排为5,8 - 二氧代-1H - 吡咯并[1,2 - a]吲哚。