کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371328 981842 2015 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Development of constrained tamoxifen mimics and their antiproliferative properties against breast cancer cells
ترجمه فارسی عنوان
توسعه تقلید تاموکسیفن و خواص ضد انعقادی آن در برابر سلول های سرطانی پستان
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

An efficient synthesis of a new series of tamoxifen mimics is described by employing iodine catalyzed ipsocyclization strategy followed by Suzuki coupling. A molecular docking studies of the synthesized compounds 11a–n and 12 in estrogen receptor (ER-α) showed that the scaffolds are fitting well in the groove, thereby suggesting them as promising antiproliferative agents for estrogen dependent breast cancer lines. All compounds were tested in vitro against breast cancer cell lines—ER positive, MCF-7; ER negative, MDA-MB-231; and control mammary epithelial cells, MEpiC. The biological results showed that most of the compounds are active against MCF-7 with IC50 values less than 6.5 μM which corroborate the results of molecular docking studies.

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 3, 1 February 2015, Pages 680–684
نویسندگان
, , , , , , , , ,