Citation: Xian Ping DAI, Xing Zhou LI, Zhi Bing ZHENG, Song LI. Synthesis and Biological Evaluation of Novel 1, 5-Diarylpyrazole-3-carboxamide Compounds as Inhibitors of ALK5[J]. Chinese Chemical Letters, ;2006, 17(5): 609-612. shu

Synthesis and Biological Evaluation of Novel 1, 5-Diarylpyrazole-3-carboxamide Compounds as Inhibitors of ALK5

1.
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016;
2.
Beijing Institute of Pharmacology & Toxicology, Beijing 100850

Received Date: 23 November 2005

Fund Project: This work was supported by the Chinese National Basic Developing Project (973 project: 2004CB518908).

Ten new 1, 5-diarylpyrazole-3-carboxamide compounds were synthesized and their structures were identified by ¹H-NMR and FAB-MS. The primary biological tests showed that compound 4j exhibited some ALK5 inhibitory activity at concentration of 1μmol/L.
- 1,
- 5-Diarylpyrazole-3-carboxamide,
- synthesis,
- inhibitors,
- ALK5
1. [1]
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2. [2]
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3. [3]
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16. [16]
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