Citation: Zeng Wu, Ming Yan, Shi-He Hu, Zhi-Cheng Yu, Yong Zhu, Ya-Dong Cheng, Hai-Chun Liu, Yan-Min Zhang, Si-Hui Yao, Wei-Fang Tang, Tao Lu. Design, synthesis and biological evaluation of indole derivatives as novel inhibitors targeting B-Raf kinase[J]. Chinese Chemical Letters, ;2014, 25(2): 351-354. shu

Design, synthesis and biological evaluation of indole derivatives as novel inhibitors targeting B-Raf kinase

Zeng Wu ^a ,
Ming Yan ^b ,
Shi-He Hu ^a ,
Zhi-Cheng Yu ^a ,
Yong Zhu ^a ,
Ya-Dong Cheng ^c ,
Hai-Chun Liu ^c ,
Yan-Min Zhang ^c ,
Si-Hui Yao ^c ,
Wei-Fang Tang ^a,, ,
Tao Lu ^d,e,,

1.
a Department of Organic Chemistry, China Pharmaceutical University, Nanjing 210009, China;
2.
b National Nanjing Center for Drug Screening, China Pharmaceutical University, Nanjing 210009, China;
3.
c Laboratory of Molecular Design and Drug Discovery, School of Sciences, China Pharmaceutical University, Nanjing 210009, China;
4.
d State Key laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China;
5.
e The Headmaster's Office, China Pharmaceutical University, Nanjing 210009, China

Corresponding author: Wei-Fang Tang, Tao Lu,
Received Date: 10 July 2013
Available Online: 18 October 2013
Fund Project: This work was financially supported by the Natural Science Foundation of Jiangsu Province (No. BK2009303) (No. BK2009303) the National Natural Science Foundation of China (No. 30973609) (No. 30973609) Fundamental Research Funds for the Central Universities (No. JKZ2011004) (No. JKZ2011004)Specialized Research Fund for the Doctoral Program of Higher Education (No. 20100096110007). (No. 20100096110007)

A series of novel indole derivatives were designed and synthesized and their inhibitory activity against B-Raf and HepG2 cell were also described. Among them, compounds 7a and 7b exhibited excellent potency, which showed the potential for further research as lead compounds.
- B-Raf kinase inhibitors,
- Receptor-based drug discovery,
- Indole derivatives,
- Biological evaluation
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沈阳化工大学材料科学与工程学院沈阳 110142