Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: lddd@benthamscience.org

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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

Affiliation: Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu 210009, China.

Keywords: 5-Amino-1H-pyrazole-4-carboxamide derivatives, Adenosine deaminase inhibitors, Antitumor, Molecular docking, ER+, MCF-7.

Graphical Abstract:


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.

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Article Details

VOLUME: 11
ISSUE: 6
Page: [749 - 755]
Pages: 7
DOI: 10.2174/1570180811666140115234123