کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1363712 981520 2009 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Crystal structure, antitumour and antimetastatic activities of disubstituted fused 1,2,4-triazinones
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Crystal structure, antitumour and antimetastatic activities of disubstituted fused 1,2,4-triazinones
چکیده انگلیسی

Molecular structure of 3,8-disubstituted 7,8-dihydroimidazo[2,1-c][1,2,4]triazin-4(6H)-ones (8–14) was confirmed by X-ray crystallography of 14. All the compounds were evaluated for their antitumour and antimetastatic activities in vitro. Furthermore, their cytotoxicities towards human normal cell line—HSF cells were established, allowing us to point out some structure–activity relationships. Among them, imidazotriazinone 12, revealing remarkable dose-dependent viability decreases in human myeloma RPMI 8226 cells, was found to be completely non-toxic towards normal HSF cells. In addition, heterobicycles 8–12 were proved to exhibit significant antimetastatic potentials in the motility assay.

Molecular structure, antitumoural and antimetastatic activities in vitro of 3,8-disubstituted 7,8-dihydroimidazo[2,1-c][1,2,4]triazin-4(6H)-ones (8–14) are presented. Among them, first of all heterobicycle 12 was found to reveal remarkable dose-dependent viability decreases in human peripheral blood myeloma RPMI 8226 cells, without affecting human normal cell line—HSF cells. Furthermore, heterobicycles 8–12 were proved to exhibit significant antimetastatic potentials in the motility assay.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 17, 1 September 2009, Pages 5095–5100
نویسندگان
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