کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1355223 980827 2011 10 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis, antitumor activity and QSAR studies of some 4-aminomethylidene derivatives of edaravone
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis, antitumor activity and QSAR studies of some 4-aminomethylidene derivatives of edaravone
چکیده انگلیسی

A series of aminomethylidene derivatives obtained from 4-formyledaravone were synthesized and characterized by IR, NMR and elemental analysis. All the compounds were screened for their antitumor activity. The compound containing 5-phenylpyrazole moiety (3q) exhibited remarkable antitumor activity in in vitro assays, especially against human breast cancer MDA-MB-361 and MDA-MB-453 cell lines. The most important whole-molecule descriptors for antitumor activity on MDA-MB-453 cells belong to the group of quantum-chemical descriptors.

Aminomethylidene derivatives obtained from 4-formyledaravone and primary amines were synthesized and tested for their antitumor activity. The compound containing 5-phenylpyrazole moiety was found to be the most active against human breast cancer MDA-MB-361 and MDA-MB-453 cell lines.Figure optionsDownload as PowerPoint slideResearch highlights
► In this work we synthesized seventeen aminomethylidene derivatives of 4-formyledaravone and investigated their antitumor activity.
► The compound containing 5-phenylpyrazole moiety is the most efficient 4-aminomethylidene derivative of edaravone against human breast cancer MDA-MB-361 and MDA-MB-453 cells.
► The most important fragmental descriptors for antitumor activity on MDA-MB-453 include the groups of quantum-chemical, topological and constitutional descriptors.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic Chemistry - Volume 39, Issue 1, February 2011, Pages 18–27
نویسندگان
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