کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1360501 981438 2008 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring
چکیده انگلیسی

We previously developed carborane-containing potent AR antagonists, BA321 and BA341, on the basis of our hypothesis that the carborane cage would be an excellent hydrophobic pharmacophore in place of steroidal C and D rings. As an extension of that work, we designed and synthesized carborane-containing AR antagonist candidates with a pyridine ring. Compound 6b, which has a pyridine ring directly bound to the p-carborane cage at the 3-position, exhibited potent AR-antagonistic activity in transcriptional activation assay using NIH3T3 cells transfected with a hAR-expression plasmid. In addition, it showed more potent antiandrogenic activity than that of the well-known antiandrogen flutamide and comparable activity to that of (R)-bicalutamide in SC-3 cell proliferation assay.

Compound 6b, which was designed based on the structures of BA321 and BA341, exhibited more potent antiandrogenic activity than that of flutamide in SC-3 cell growth inhibition assay.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 17, 1 September 2008, Pages 8022–8028
نویسندگان
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