کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2474637 1113153 2011 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis and antitumor activity of C3/C3 bis-fluoroquonolones cross-linked with [1,2,4]triazolo[3,4-b] [1,3,4]thiadiazole
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی اکتشاف دارویی
پیش نمایش صفحه اول مقاله
Design, synthesis and antitumor activity of C3/C3 bis-fluoroquonolones cross-linked with [1,2,4]triazolo[3,4-b] [1,3,4]thiadiazole
چکیده انگلیسی

To contribute to the development of an efficient method for the conversion of antibacterial fluoroquinolones to antitumor fluoroquinolones, a series of C3/C3 bis-fluoroquinolone fused heterocycles cross-linked with a [1,2,4]-triazolo[3,4-b] [1,3,4]-thiadiazole core as a common bioisostere of two carboxylic acid groups was designed and synthesized as their hydrochloride salts. Structures were characterized by elemental analysis and spectral data and their in vitro antitumor activity against L1210, CHO and HL60 cell lines was screened by determination of their IC50 values in the methylthiazole trazolium (MTT) assay. Two compounds were highly potent against the HL60 cell line and represent promising lead compounds for future development.

A series of C3/C3 bis-fluoroquinolone fused heterocycles cross-linked with a [1,2,4]-triazolo[3,4-b] [1,3,4]-thiadiazole core as a common bioisostere of two carboxylic acid groups was designed and synthesized. Their in vitro antitumor activities against L1210, CHO and HL60 cell lines were screened by determination of their IC50 values in the methylthiazole trazolium (MTT) assay.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Acta Pharmaceutica Sinica B - Volume 1, Issue 3, October 2011, Pages 172–177
نویسندگان
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