Weinkauf R L, Chen A Y, Yu C, Liu L, Barrows L, LaVoie E J
Department of Pharmaceutical Chemistry, College of Pharmacy, Rutgers, State University of New Jersey, Piscataway 08855.
Bioorg Med Chem. 1994 Aug;2(8):781-6. doi: 10.1016/s0968-0896(00)82177-x.
Substituted pyrido[3,4-b]carbazoles, pyrido[2,3-b]carbazoles, indolo[2,3-b]quinolines, and benzimidazo[1,2-b]-isoquinolines were synthesized and evaluated for biological activity. Several methylated derivatives of these heterocyclic compounds had similar activity to ellipticine as mammalian topoisomerase II inhibitors. Methylated derivatives of these heterocyclic compounds were also highly active in vitro, inhibiting the growth of several human tumor cell lines. These data demonstrate that the antineoplastic activity associated with ellipticine can be retained within a wide variety of analogous heterocyclics.
合成了取代吡啶并[3,4 - b]咔唑、吡啶并[2,3 - b]咔唑、吲哚并[2,3 - b]喹啉和苯并咪唑并[1,2 - b]异喹啉，并对其生物活性进行了评估。这些杂环化合物的几种甲基化衍生物作为哺乳动物拓扑异构酶II抑制剂，具有与椭圆玫瑰树碱相似的活性。这些杂环化合物的甲基化衍生物在体外也具有高活性，能抑制多种人类肿瘤细胞系的生长。这些数据表明，与椭圆玫瑰树碱相关的抗肿瘤活性可以在多种类似杂环化合物中得以保留。
