کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10596024 | 981892 | 2013 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
MMP inhibition by barbiturate homodimers
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: MMP inhibition by barbiturate homodimers MMP inhibition by barbiturate homodimers](/preview/png/10596024.png)
چکیده انگلیسی
We have studied some homodimeric compounds derived from 5-homopiperazine substituted pyrimidine triones (barbiturates) with linkers in the range 2-20 carbon atoms. The compounds were designed to be capable of resisting absorption, to be stable in the gut and to maintain inhibitory potency against gelatinases and related function.The compounds were then assessed for inhibitory potency against a panel of MMPs (1, 2, 8, 9 and 13). The dimer compounds had similar potency and selectivity to the homopiperazine barbiturate monomer class. At 100Â nM, selected dimers significantly inhibited cancer cell invasion in a matrigel assay using Caco-2 cells stimulated by hepatic growth factor. Finally, selected dimers showed adequate stability in simulated intestinal fluid to suggest the capacity to transit to the colon.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 2, 15 January 2013, Pages 444-447
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 2, 15 January 2013, Pages 444-447
نویسندگان
Jun Wang, Marek W. Radomski, Carlos Medina, John F. Gilmer,