作为拓扑异构酶I抑制剂的1,5-萘啶的合成及生物学评价。一类新型抗增殖剂。
Synthesis and biological evaluation of 1,5-naphthyridines as topoisomerase I inhibitors. A new family of antiproliferative agents.
作者信息
Alonso Concepción, Fuertes María, González María, Rodríguez-Gascón Alicia, Rubiales Gloria, Palacios Francisco
机构信息
Departamento de Quimica Organica I and Centro de Investigacion Lascaray (Lascaray Research Center), Facultad de Farmacia, Universidad del Pais Vasco/Euskal Herriko Unibertsitatea (UPV/EHU), Paseo de la Universidad 7, 01006 Vitoria- Gasteiz, Spain.
出版信息
Curr Top Med Chem. 2014;14(23):2722-8. doi: 10.2174/1568026614666141215152441.
The synthesis of a variety of phenyl- and indeno-1,5-naphthyridine derivatives as new substrates with anticancer activity is described. Several of the prepared products were addressed to in vitro anticancer screening which indicated that some of them exhibited inhibitory effect of Top1 and antiproliferative activity against human colon cancer cells (COLO 205).
描述了多种具有抗癌活性的新型底物——苯基和茚并[1,5]萘啶衍生物的合成。对几种制备的产物进行了体外抗癌筛选，结果表明其中一些表现出对Top1的抑制作用以及对人结肠癌细胞（COLO 205）的抗增殖活性。
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