Medicinal Chemistry : ELSEVIER ; Design and synthesis of novel 2,4-diaryl-5H-indeno[1,2-ь]pyridine derivatives, and their evaluation of topoisomerase inhibitory activity and cytotoxicity = Medicinal Chemistry : ELSEVIER ; Design and synthesis of novel 2,4-diaryl-5H-indeno[1,2-ь]pyridine derivatives, and their evaluation of topoisomerase inhibitory activity and cytotoxicity

다국어 초록 (Multilingual Abstract)

For the development of potential anticancer agents, We designed and synthesized 30 new 2,4-diaryl-5H-indeno[1,2-ь]pyridine derivatives containing aryl moiery such as furyl, thienyl, Pyridyl, and phenyl at 2-and 4-position of 5H-indeno[1,2-ь]pyridine. They were avaluated for topoisomerase I and ll inhibitory activity, and cytotoxicity against several human cancer cell lines. Among prepared 30 compounds, 7,8,9,10,12,14,16,19,20,22, and 23 with 2-or 3-thienyl either at 2-or 4-position of central pyridine showed the significant or moderate topoisomerase ll inhibitory activity. Compoumds 7,8,11,12,13, and 22 with 2-furyl, 2-thienyl or 3-thienyl at 2-position of central pyridine showed the significant or moderate topoisomerase I inhibitory activity. Especially. compound 12 with strong topoisomerase ll inhibitory activity at 100 um and 20 um. and moderate topoisomerase I inhibitory activity displayed strong cytotoxicity against several human cancer cell lines. ⓒ 2014 Elsevier Ltd. All rights reserved.