کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374614 | 981922 | 2010 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Proline isosteres in a series of 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitors of IGF-1R kinase and IR kinase
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Pyrrolidine, pyrrolidinone, carbocyclic, and acyclic groups were used as isosteric proline replacements in a series of insulin-like growth factor I receptor kinase/insulin receptor kinase inhibitors. Examples that were similar in potency to proline-containing reference compounds were shown to project a key fluoropyridine amide into a common space, while less potent compounds were not able to do so for reasons of stereochemistry or structural rigidity.
Analogs utilizing proline isosteres in IGF-1R/IR inhibitors are disclosed. X-ray co-crystallography of selected analogs reveals information key to target potency.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 17, 1 September 2010, Pages 5027–5030
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 17, 1 September 2010, Pages 5027–5030
نویسندگان
Anthony J. Sampognaro, Mark D. Wittman, Joan M. Carboni, Chiehying Chang, Ann F. Greer, Warren W. Hurlburt, John S. Sack, Dolatrai M. Vyas,