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

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

Volume: 11 Issue: 6

Author(s): Baowei Yang, Wukun Liu, Yicheng Mei, Dandan Huang, Hai Qian, Wenlong Huang and Ronald Gust

Affiliation:

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

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.

Cite this article as:

Yang Baowei, Liu Wukun, Mei Yicheng, Huang Dandan, Qian Hai, Huang Wenlong and Gust Ronald, Design, Synthesis and Biological Evaluation of 5-Amino-1H-pyrazole-4- carboxamide Derivatives as Potential Antitumor Agents, Letters in Drug Design & Discovery 2014; 11 (6) . https://dx.doi.org/10.2174/1570180811666140115234123

DOI https://dx.doi.org/10.2174/1570180811666140115234123	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X