کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375095 | 981932 | 2010 | 4 صفحه PDF | دانلود رایگان |
In continuation of our efforts toward hit identification and optimization for a B-Raf kinase project, we have employed a scaffold hopping strategy. The original HTS hit scaffold pyrazolo[1,5-a]pyrimidine was replaced with different thienopyrimidine and thienopyridine scaffolds to append the optimal pharmacophore moieties in order to generate novel B-raf kinase inhibitors with desirable potency and properties. This strategy led to the identification of additional lead compound 11b which had good enzyme and cell potency, while maintaining selectivity over a number of kinases.
Scaffold hopping strategy was employed to replace the HTS hit scaffold pyrazolo[1,5-a]pyrimidine. This strategy led to the identification of additional lead compound 11b with enhanced enzyme and cellular potency, while maintaining good selectivity over a number of kinases.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 8, 15 April 2010, Pages 2431–2434