کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1395954 | 1501169 | 2012 | 8 صفحه PDF | دانلود رایگان |
A series of pyrimido[5,4-c]quinoline-4-(3H)-one derivatives variously substituted at positions 2 and 3 were synthesized and evaluated for their in vitro antiproliferative activities against a panel of six human cancer cell lines. Biological evaluation revealed that the vast majority of derivatives exhibited moderate tumor growth inhibitory activities. In particular, compound 7e showed effective anti-tumor activity with broad-spectrum toward numerous cell lines and the most active member in this study. This derivative displaying significant activity against KB (IC50: 4.9 μM), CNE2 (IC50: 13.8 μM), MGC-803 (IC50: 4.8 μM), GLC-82 (IC50: 7.88 μM), MDA-MB-453 (IC50: 18.2 μM) and MCF-7 (IC50: 10.1 μM) cell lines could be considered as the most promising and useful template for future development to obtain more potent anti-tumor agent(s).
A series of pyrimido[5,4-c]quinoline-4-(3H)-one derivatives variously substituted at positions 2 and 3 were synthesized and evaluated for their in vitro antiproliferative activities.Figure optionsDownload as PowerPoint slideHighlights
► Twenty-five pyrimido[5,4-c]quinoline-4-(3H)-one derivatives were synthesized.
► Some new compounds exhibited potent anti-proliferative activities.
► Preliminary structure-activity relationships were revealed.
Journal: European Journal of Medicinal Chemistry - Volume 47, January 2012, Pages 206–213