کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1373591 981903 2007 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Identification of a series of tetrahydroisoquinoline derivatives as potential therapeutic agents for breast cancer
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Identification of a series of tetrahydroisoquinoline derivatives as potential therapeutic agents for breast cancer
چکیده انگلیسی

A series of tetrahydroisoquinoline-N-phenylamide derivatives were designed, synthesized, and tested for their relative binding affinities, and antagonistic activities against estrogen receptor (ER). Compound 1f (relative binding affinity, RBA = 5) showed higher binding affinity than tamoxifen (RBA=1), a potent ER antagonist and currently being used for breast cancer therapy. Compound 1f also exerted optimal antagonistic activity against ER in reporter and cell proliferation assays. Interestingly, compound 1j, which only has a minor agonistic effect against ER, acted as a progesterone receptor (PR) antagonist and exerted agonistic activity against AP-1 through ER pathway. Our results show that these new compounds can be employed as leading pharmacophore for further development of potent selective ER and/or PR modulators or antagonists.

The synthesis and evaluation of 1,2,3,4-tetrahydroisoquinoline-N-phenylamide derivatives as estrogen receptor antagonists are reported.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 9, 1 May 2007, Pages 2581–2589
نویسندگان
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