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B-Raf kinase inhibitors: hit enrichment through scaffold hopping.

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Gopalsamy A,Shi M,Hu Y,Lee F,Feldberg L,Frommer E,Kim S,Collins K,Wojciechowicz D,Mallon R

doi

10.1016/j.bmcl.2010.03.030

subject

Has Abstract

pub_date

2010-04-15 00:00:00

pages

2431-4

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00351-3

journal_volume

20

pub_type

杂志文章

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