Abstract
17α-Hydroxylase/17,20-lyase is a target in the treatment of hormone-dependent prostate cancer. Here we report the results of a study into a range of alkanesulfonate derivatives of 4-hydroxybenzylimidazole which show the compounds to be good inhibitors with 5 [IC50=1.11µM (17α-OHase) and IC50=1.28µM (lyase)] being the most potent but weaker than ketoconazole.
Keywords: 17α-hydroxylase/17, 17α-OHase, 20-lyase, Azole, Inhibitors Lyase.
Letters in Drug Design & Discovery
Title:Synthesis and Biochemical Evaluation of a Range of 4-(n-alkanesulfonate) benzyl Imidazole-Based Compounds as Inhibitors of Rat Testicular 17α-hydroxylase/17,20-lyase (P45017α) in the Treatment of Hormone- Dependent Prostate Cancer
Volume: 11 Issue: 8
Author(s): Pallav S. Shah, Imran Shahid, Wai-Yee Lee, Caroline P. Owen and Sabbir Ahmed
Affiliation:
Keywords: 17α-hydroxylase/17, 17α-OHase, 20-lyase, Azole, Inhibitors Lyase.
Abstract: 17α-Hydroxylase/17,20-lyase is a target in the treatment of hormone-dependent prostate cancer. Here we report the results of a study into a range of alkanesulfonate derivatives of 4-hydroxybenzylimidazole which show the compounds to be good inhibitors with 5 [IC50=1.11µM (17α-OHase) and IC50=1.28µM (lyase)] being the most potent but weaker than ketoconazole.
Export Options
About this article
Cite this article as:
Shah S. Pallav, Shahid Imran, Lee Wai-Yee, Owen P. Caroline and Ahmed Sabbir, Synthesis and Biochemical Evaluation of a Range of 4-(n-alkanesulfonate) benzyl Imidazole-Based Compounds as Inhibitors of Rat Testicular 17α-hydroxylase/17,20-lyase (P45017α) in the Treatment of Hormone- Dependent Prostate Cancer, Letters in Drug Design & Discovery 2014; 11 (8) . https://dx.doi.org/10.2174/1570180811666131230235538
DOI https://dx.doi.org/10.2174/1570180811666131230235538 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
A Family of Pleiotropically Acting MicroRNAs in Cancer Progression, miR-200: Potential Cancer Therapeutic Targets
Current Pharmaceutical Design Neuroimaging of the Serotonin Transporter: Possibilities and Pitfalls
Current Psychiatry Reviews Endothelin-1 Actions on Vascular Smooth Muscle Cell Functions As a Target for the Prevention of Atherosclerosis
Current Vascular Pharmacology Models of Infection Before and After Stroke: Investigating New Targets
Infectious Disorders - Drug Targets Endoradiotherapy with Peptides - Status and Future Development
Current Medicinal Chemistry Genistein Affects Expression of Cytochrome P450 (CYP450) Genes in Hepatocellular Carcinoma (HEPG2/C3A) Cell Line
Drug Metabolism Letters RNA Silencing: Recent Developments on miRNAs
Recent Patents on DNA & Gene Sequences Flavonoids Influence Epigenetic-Modifying Enzyme Activity: Structure-Function Relationships and the Therapeutic Potential for Cancer
Current Medicinal Chemistry Metabolic Alterations in Renal and Prostate Cancer
Current Drug Metabolism Evolving Insights into the Pathophysiology of Diabetic Neuropathy: Implications of Malfunctioning Glia and Discovery of Novel Therapeutic Targets
Current Pharmaceutical Design Synthesis and Biological Evaluation of a Novel Apogossypolone Derivative
Letters in Drug Design & Discovery Somatostatin, Somatostatin Analogs and Somatostatin Receptor Dynamics in the Biology of Cancer Progression
Current Molecular Medicine Polo-like Kinase 1-targeting Chitosan Nanoparticles Suppress the Progression of Hepatocellular Carcinoma
Anti-Cancer Agents in Medicinal Chemistry Molecular Signatures of Biomarkers in Cancer Development, Diagn osis, and its Prognostic Accuracy
Current Biomarkers (Discontinued) Retinoids in Clinical Use
Medicinal Chemistry “Smart” Nanocarriers: A New Paradigm for Tumor Targeting Drug Delivery Systems
Drug Delivery Letters Nanoliposomal Encapsulation Enhances In Vivo Anti-Tumor Activity of Niclosamide against Melanoma
Anti-Cancer Agents in Medicinal Chemistry ADDENDUM: Increased Akt Signaling Resulting from the Loss of Androgen Responsiveness in Prostate Cancer. Dulinska-Litewka J, McCubrey JA, Laidler P. Curr. Med. Chem., 2013, 20(1), 144-157.
Current Medicinal Chemistry Renin-angiotensin System Blockers and Modulation of Radiation-Induced Brain Injury
Current Drug Targets Unlocking the Molecular Mechanisms of DNA Repair and Platinum Drug Resistance in Cancer Chemotherapy
Current Drug Therapy