کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10598166 | 982011 | 2005 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors](/preview/png/10598166.png)
چکیده انگلیسی
Tetrahydroquinoline-based small molecule inhibitors of farnesyltransferase (FT) have been identified. Lead compounds were shown to have nanomolar to sub-nanomolar activity in biochemical assays with excellent potency in a Ras-mutated cellular reversion assay. BMS-316810 (9e), a 0.7Â nM FT inhibitor, was orally-active in a nude mouse tumor allograft efficacy study.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 7, 1 April 2005, Pages 1895-1899
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 7, 1 April 2005, Pages 1895-1899
نویسندگان
Louis J. Lombardo, Amy Camuso, John Clark, Krista Fager, Johnni Gullo-Brown, John T. Hunt, Ivan Inigo, David Kan, Barry Koplowitz, Francis Lee, Kelly McGlinchey, Ligang Qian, Carolyn Ricca, George Rovnyak, Sarah Traeger, John Tokarski, David K. Williams,