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Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
Epub Full Text Article
DOI: 10.2174/1570180811666140115234123      Price:  $95

Design, Synthesis and Biological Evaluation of 5-Amino-1H-pyrazole-4-carboxamide Derivatives as Potential Antitumor Agents

Author(s): Baowei Yang, Wukun Liu, Yicheng Mei, Dandan Huang, Hai Qian, Wenlong Huang and Ronald Gust
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.
5-Amino-1H-pyrazole-4-carboxamide derivatives, Adenosine deaminase inhibitors, Antitumor, Molecular docking, ER+, MCF-7
Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu 210009, China.