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Anti-Cancer Agents in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Research Article

Design, Synthesis and Biological Evaluation of 1-methyl-1H-pyrazole-5-Carboxamide Derivatives as Novel Anti-Prostate Cancer Agents

Author(s): Xin Chen , Changqing Xu, Yuxia Li, Xiaoming Duan and Guisen Zhao*

Volume 21 , Issue 17 , 2021

Published on: 02 February, 2021

Page: [2368 - 2378] Pages: 11

DOI: 10.2174/1871520621666210202162953

Price: $65

Abstract

Background: The Androgen Receptor (AR) signaling functionis a critical driving force for the progression of Prostate Cancer (PCa) to bring about anti-prostate cancer agents, and AR has been proved to be an effective therapeutic target even for Castration-Resistant Prostate Cancer (CRPC). Objective: In order to discover novel anti-prostate cancer agents, we performed structural modifications based on the lead compounds T3 and 10e.

Methods: A set of 1-methyl- 1H-pyrazole-5-carboxamide derivatives were synthesized and evaluated for their inhibitory activities against both expressions of Prostate-Specific Antigen (PSA) and growth of PCa cell lines.

Results: Compound H24 was found to be able to completely block PSA expression at 10μM, and showed prominent antiproliferative activity in both the LNCaP cell line (GI50 = 7.73μM) and PC-3 cell line (GI50 = 7.07μM).

Conclusion: These preliminary data supported a further evaluation of compound H24 as a potential agent to treat prostate cancer.

Keywords: Androgen receptor, prostate cancer, pyrazole derivatives, prostate-specific antigen, antiproliferative activity, structural modification.

Graphical Abstract

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