Alonso Concepción, Fuertes María, González María, Rubiales Gloria, Tesauro Cinzia, Knudsen Birgitta R, Palacios Francisco
Departamento de Química Orgánica I, Facultad de Farmacia and Centro de Investigación Lascaray (Lascaray Research Center), Universidad del País Vasco/Euskal Herriko Unibertsitatea (UPV/EHU), Paseo de la Universidad 7, 01006, Vitoria-Gasteiz, Spain.
Department of Molecular Biology and Genetics and Interdisciplinary Nanoscience Center (iNANO), Aarhus University, Aarhus, 8000, Denmark.
Eur J Med Chem. 2016 Jun 10;115:179-90. doi: 10.1016/j.ejmech.2016.03.031. Epub 2016 Mar 14.
In an effort to establish new candidates with improved anticancer activity, we report here the synthesis of various series of 7H-indeno[2,1-c][1,5]-naphthyridines and novel 7H-indeno[2,1-c][1,5]-naphthyridine-7-ones and 7H-indeno[2,1-c][1,5]-naphthyridine-7-ols. Most of the products which were synthesized were able to inhibit Topoisomerase I activity. Moreover, in vitro testing demonstrated that a subset of the products exhibited a cytotoxic effect on cell lines derived from human breast cancer (BT 20), human lung adenocarcinoma (A 549), or human ovarian carcinoma (SKOV3).
为了开发具有更强抗癌活性的新候选药物，我们在此报告各种系列的7H-茚并[2,1-c][1,5]萘啶以及新型7H-茚并[2,1-c][1,5]萘啶-7-酮和7H-茚并[2,1-c][1,5]萘啶-7-醇的合成。所合成的大多数产物能够抑制拓扑异构酶I的活性。此外，体外测试表明，部分产物对源自人乳腺癌（BT 20）、人肺腺癌（A 549）或人卵巢癌（SKOV3）的细胞系具有细胞毒性作用。
