Szumilak Marta, Galdyszynska Malgorzata, Dominska Kamila, Bak-Sypien Irena I, Merecz-Sadowska Anna, Stanczak Andrzej, Karwowski Boleslaw T, Piastowska-Ciesielska Agnieszka W
Department of Hospital Pharmacy, Faculty of Pharmacy, Medical University of Lodz, 1 Muszynskiego Street, 90-151 Lodz, Poland.
Department of Comparative Endocrinology, Medical University of Lodz, 7/9 Zeligowskiego Street, 90-752 Lodz, Poland.
Molecules. 2017 May 12;22(5):794. doi: 10.3390/molecules22050794.
Polyamine conjugates with bicyclic terminal groups including quinazoline, naphthalene, quinoline, coumarine and indole have been obtained and their cytotoxic activity against PC-3, DU-145 and MCF-7 cell lines was evaluated in vitro. Their antiproliferative potential differed markedly and depended on both their chemical structure and the type of cancer cell line. Noncovalent DNA-binding properties of the most active compounds have been examined using ds-DNA thermal melting studies and topo I activity assay. The promising biological activity, DNA intercalative binding mode and favorable drug-like properties of bis(naphthalene-2-carboxamides) make them a good lead for further development of potential anticancer drugs.
已获得具有双环端基（包括喹唑啉、萘、喹啉、香豆素和吲哚）的多胺缀合物，并在体外评估了它们对PC-3、DU-145和MCF-7细胞系的细胞毒性活性。它们的抗增殖潜力差异显著，并且取决于其化学结构和癌细胞系的类型。使用双链DNA热变性研究和拓扑异构酶I活性测定法研究了最具活性化合物的非共价DNA结合特性。双（萘-2-甲酰胺）具有良好的生物活性、DNA插入结合模式和良好的类药物性质，使其成为进一步开发潜在抗癌药物的良好先导化合物。
