کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1364892 | 981548 | 2007 | 20 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and synthesis of piperidine farnesyltransferase inhibitors with reduced glucuronidation potential
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The design and synthesis of a novel piperidine series of farnesyltransferase (FTase) inhibitors with reduced potential for metabolic glucuronidation are described. The various substitution and exchange of the phenyl group at the C-2 position of the previously described 2-(4-hydroxy)phenyl-3-nitropiperidine 1a (FTase IC50 = 5.4 nM) resulted in metabolically stable compounds with potent FTase inhibition (14a IC50 = 4.3 nM, 20a IC50 = 3.0 nM, and 50a IC50 = 16 nM). Molecular modeling studies of these compounds complexed with FTase and farnesyl pyrophosphate are also described.
Metabolically stable compound 20a with potent FTase inhibition (IC50 = 3 nM) is reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 3, 1 February 2007, Pages 1363–1382
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 3, 1 February 2007, Pages 1363–1382
نویسندگان
Rieko Tanaka, Almudena Rubio, Nancy K. Harn, Douglas Gernert, Timothy A. Grese, Jun Eishima, Mitsunobu Hara, Nobuyuki Yoda, Rui Ohashi, Takashi Kuwabara, Shiro Soga, Shiro Akinaga, Shinji Nara, Yutaka Kanda,