Abstract
It has been demonstrated that taspine derivatives act as anticancer agents, thus we designed and synthesized a novel class of symmetrical biphenyl derivatives. We evaluated the cytotoxicity and antitumor activity of biphenyls against five human tumor and normal cell lines. The results indicated that the majority of the compounds exhibited anticancer activity equivalent to or greater than the positive control. Compounds (11) and (12) demonstrated the most potent cytotoxic activity with IC50 values between 19.41 μM and 29.27 μM. The potent antiproliferative capabilities of these compounds against ECV304 human transformed endothelial cells indicated that these biphenyls could potentially serve as antiangiogenic agents. We also reviewed the relationship between structure and activity based on the experimental results. Our findings provide a good starting point for further development of symmetrical biphenyl derivatives as potential novel anticancer agents.
Keywords: Symmetrical taspine derivatives, antiproliferative activity, cytotoxicity, anticancer agents, antiangiogenic agents, VEGFR-2, biphenyl derivatives, antitumor, IC50, endothelial cells, structure and activity
Medicinal Chemistry
Title: Synthesis and Cytotoxic Evaluation of Novel Symmetrical Taspine Derivatives as Anticancer Agents
Volume: 7 Issue: 4
Author(s): Jie Zhang, Yanmin Zhang, Xiaoyan Pan, Sicen Wang and Langchong He
Affiliation:
Keywords: Symmetrical taspine derivatives, antiproliferative activity, cytotoxicity, anticancer agents, antiangiogenic agents, VEGFR-2, biphenyl derivatives, antitumor, IC50, endothelial cells, structure and activity
Abstract: It has been demonstrated that taspine derivatives act as anticancer agents, thus we designed and synthesized a novel class of symmetrical biphenyl derivatives. We evaluated the cytotoxicity and antitumor activity of biphenyls against five human tumor and normal cell lines. The results indicated that the majority of the compounds exhibited anticancer activity equivalent to or greater than the positive control. Compounds (11) and (12) demonstrated the most potent cytotoxic activity with IC50 values between 19.41 μM and 29.27 μM. The potent antiproliferative capabilities of these compounds against ECV304 human transformed endothelial cells indicated that these biphenyls could potentially serve as antiangiogenic agents. We also reviewed the relationship between structure and activity based on the experimental results. Our findings provide a good starting point for further development of symmetrical biphenyl derivatives as potential novel anticancer agents.
Export Options
About this article
Cite this article as:
Zhang Jie, Zhang Yanmin, Pan Xiaoyan, Wang Sicen and He Langchong, Synthesis and Cytotoxic Evaluation of Novel Symmetrical Taspine Derivatives as Anticancer Agents, Medicinal Chemistry 2011; 7 (4) . https://dx.doi.org/10.2174/157340611796150914
DOI https://dx.doi.org/10.2174/157340611796150914 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...read more
- 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
-
Interplay between Epigenetics & Cancer Metabolism
Current Pharmaceutical Design Phosphonomethoxyalkyl Analogs of Nucleotides
Current Pharmaceutical Design Radiolabeled Oligonucleotides for Antisense Imaging
Current Organic Synthesis Autologous Mesenchymal Stem Cell Therapy in Progressive Multiple Sclerosis: An Open Label Study
Current Stem Cell Research & Therapy Brain Permeable Nanoparticles
Recent Patents on CNS Drug Discovery (Discontinued) Irradiation Toxicity and Inflammatory Bowel Diseases (IBD): Review
Reviews on Recent Clinical Trials Gedunin, A Neem Limonoid in Combination with Epalrestat Inhibits Cancer Hallmarks by Attenuating Aldose Reductase-Driven Oncogenic Signaling in SCC131 Oral Cancer Cells
Anti-Cancer Agents in Medicinal Chemistry Bringing Light into the Diagnosis of Skin Disorders - Short Review on Laser Induced Fluorescence Spectroscopy and Optical Coherence Tomography in Dermatology
Current Medical Imaging Molecular Pathways Linking Inflammation and Cancer
Current Molecular Medicine Methylaervine as Potential Lead Compound Against Cervical Carcinoma: Pharmacologic Mechanism Prediction based on Network Pharmacology
Current Computer-Aided Drug Design Protein Bioinformatics Applied to Virology
Current Protein & Peptide Science Nanomedicine for Cancer Therapy Using Autophagy: An Overview
Current Topics in Medicinal Chemistry Tubulin Inhibitors: A Patent Survey
Recent Patents on Anti-Cancer Drug Discovery Editorial (Hot Topic: Cancer Imaging: Progress and Prospect)
Current Molecular Imaging (Discontinued) <i>In Vivo</i> Anti-Tumor Effects of Flavokawain A in 4T1 Breast Cancer Cell-Challenged Mice
Anti-Cancer Agents in Medicinal Chemistry Complications of Paget Bone Disease: A Study of 69 Patients
Current Rheumatology Reviews The Effect of Resveratrol on the Werner Syndrome RecQ Helicase Gene and Telomerase Activity
Current Aging Science Withdrawal Notice: Circulatory Cells as Tumortropic Carrier for Targetability Improvement
Current Drug Delivery Arsenic trioxide Alters the MicroRNA Expression Profile of U87 glioblastoma
Anti-Cancer Agents in Medicinal Chemistry Clonetics
Current Drug Metabolism