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.
Anti-Cancer Agents in Medicinal Chemistry
Title:Design, Synthesis and Biological Evaluation of 1-methyl-1H-pyrazole-5-Carboxamide Derivatives as Novel Anti-Prostate Cancer Agents
Volume: 21 Issue: 17
Author(s): Xin Chen , Changqing Xu, Yuxia Li, Xiaoming Duan and Guisen Zhao*
Affiliation:
- Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Jinan 250012, Shandong,China
Keywords: Androgen receptor, prostate cancer, pyrazole derivatives, prostate-specific antigen, antiproliferative activity, structural modification.
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.
Export Options
About this article
Cite this article as:
Chen Xin , Xu Changqing , Li Yuxia, Duan Xiaoming and Zhao Guisen*, Design, Synthesis and Biological Evaluation of 1-methyl-1H-pyrazole-5-Carboxamide Derivatives as Novel Anti-Prostate Cancer Agents, Anti-Cancer Agents in Medicinal Chemistry 2021; 21(17) . https://dx.doi.org/10.2174/1871520621666210202162953
DOI https://dx.doi.org/10.2174/1871520621666210202162953 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |

- Author Guidelines
- Editorial Policies
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Allegations from Whistleblowers
- Publishing Ethics and Rectitude
- Increase Visibility Of Your Article
- Archiving Policies
- Reviewer Guidelines
- Guest Editor Guidelines
- Board Recruitment Workflow
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Announcements
- Forthcoming Thematic Issues
Related Articles
-
Ligand-receptor Engineering and its Application Towards the Complementation of Genetic Disease and Target Identification
Current Topics in Medicinal Chemistry Signal Transduction Pathway Regulated by Genistein and its Therapeutic Use
Current Signal Transduction Therapy Recent Pharmacoproteomics Studies of Warfarin in the Asia-Pacific: A New Strategy for Personalized Medicine?
Current Pharmacogenomics and Personalized Medicine Regulation of the DNA Damage Response to DSBs by Post-Translational Modifications
Current Genomics Meet Our Editorial Board Member:
Current Cancer Drug Targets Cancer Molecular Imaging: Radionuclide-Based Biomarkers of the Epidermal Growth Factor Receptor (EGFR)
Current Topics in Medicinal Chemistry Advances in the Physiology of GPR55 in the Central Nervous System
Current Neuropharmacology Gallium in Cancer Treatment
Current Topics in Medicinal Chemistry The Mechanism of Calcitriol in Cancer Prevention and Treatment
Current Medicinal Chemistry The Use of Innovative Tools to Reproduce Human Cancer Translocations: Lessons from the CRISPR/Cas System
Current Biotechnology Cytopathological Mechanisms in Mitochondrial Disease
Current Chemical Biology Immunobiology of Antigen-Specific Immunoglobulin Free Light Chains in Chronic Inflammatory Diseases
Current Pharmaceutical Design Hypertension, Anti-Hypertensive Therapy and Neoplasia
Current Pharmaceutical Design Experience with Androgen Deprivation Therapy for Prostate Cancer in Japan and Future Perspectives
Current Cancer Drug Targets Anti-Angiogenic Effects of Resveratrol on Cerebral Angiogenesis
Current Neurovascular Research Discovery and Clinical Development of Dutasteride, a Potent Dual 5α- Reductase Inhibitor
Current Topics in Medicinal Chemistry Recent Advances in Artemisinin Production Through Heterologous Expression
Current Medicinal Chemistry Can an Apple a Day Keep the Doctor Away?
Current Pharmaceutical Design FDG-PET/CT and SPECT/CT in Oncology
Current Medical Imaging Antigenic Peptide Vaccination: Provoking Immune Response and Clinical Benefit for Cancer
Current Immunology Reviews (Discontinued)