Design, Synthesis and Biological Evaluation of 5-Amino-1H-pyrazole-4- carboxamide Derivatives as Potential Antitumor Agents
Baowei Yang, Wukun Liu, Yicheng Mei, Dandan Huang, Hai Qian, Wenlong Huang and Ronald Gust
Affiliation: Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu 210009, China.
Adenosine deaminase (ADA) inhibitors have been found to have antitumor activities. Here, thirteen potential
adenosine deaminase inhibitors 5-amino-1H-pyrazole-4-carboxamide derivatives were designed, synthesized and screened
for antitumor activities. Compound 8e exhibited strong growth-inhibitory effects which showed selectivity toward the estrogen
receptor positive breast cancer cells (MCF-7) compared to other 5-amino-1H-pyrazole-4-carboxamide derivatives.
In addition, it also exhibited appropriate (μM) adenosine deaminase inhibitory potency. Preliminary structure-activity relationships
indicated that the incorporation of long chain branching on nitrogen atoms at pyrazole moiety was responsible
for their activity.
Keywords: 5-Amino-1H-pyrazole-4-carboxamide derivatives, Adenosine deaminase inhibitors, Antitumor, Molecular docking,
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