کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1396383 1501187 2010 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Trifluoromethyl-promoted homocamptothecins: Synthesis and biological activity
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Trifluoromethyl-promoted homocamptothecins: Synthesis and biological activity
چکیده انگلیسی

The homocamptothecin (hCPT) represents a new class of topoisomerase inhibitor which combines enhanced plasma stability and strong antitumor activity. Fluorine imparts desirable characteristics to drugs by modulating both the pharmacokinetics and pharmacodynamic properties of a drug. Therefore, in an attempt to improve the antitumor activity of homocamptothecins, seven new 7-trifluoromethylated homocamptothecin derivatives were prepared by proline-catalyzed Friedlander annulation. The antitumor activity in vitro and in vivo on cancer cell lines, and inhibitory properties of topoisomerase I-mediated DNA cleavage of compounds 6c and 8b were evaluated. Several of these trifluoromethylated hCPT derivatives (such as 6a, 6b and 6c) possessed higher in vitro antitumor activity than topotecan (TPT). Especially, the compound 6c showed effective in vivo antitumor activity comparable to that of TPT.

Seven new 7-trifluoromethylated homocamptothecin derivatives were prepared firstly by proline-catalyzed Friedlander annulation. Several of these fluorinated derivatives possessed higher antitumor activities than Topotecan (TPT).Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 7, July 2010, Pages 2726–2732
نویسندگان
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