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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

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Author(s): Baowei Yang, Wukun Liu, Yicheng Mei, Dandan Huang, Hai Qian, Wenlong Huang and Ronald Gust
Abstract:
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, ER+, MCF-7
Affiliation:
Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu 210009, China.