Abstract
Glioblastoma Multiforme (GBM) continues to demand improved chemotherapeutic solutions. In order to discover novel chemotherapeutic agents for GBM, we identified novel tetrahydroisoquinoline (THI) analogs as antiglioma agents. The present study reports the design, synthesis and in vitro evaluation of new THI derivatives in four established human glioma cell lines (T98, U87, LN18 and A172). Our structure activity relationship (SAR) studies revealed that the important modification of the carbon linker between the biphenyl and THI ring yielded EDL-360 (12) as a potent antiglioma agent (LN18; IC50: 5.42 ±0.06 μM) and is considered to be our new lead drug candidate for further preclinical studies.
Keywords: Antiglioma activity, EDL-155 analogs, glioblastoma multiforme (GBM), tetrahydroisoquinoline (THI).
Anti-Cancer Agents in Medicinal Chemistry
Title:Synthesis and In Vitro Evaluation of Novel 1,2,3,4-Tetrahydroisoquinoline Derivatives as Potent Antiglioma Agents
Volume: 14 Issue: 3
Author(s): Renukadevi Patil, Amira Hosni-Ahmed, Terreia S. Jones, Shivaputra A. Patil, Likeselam B. Asres, Xiangdi Wang, Ryan C. Yates, Eldon E. Geisert and Duane D. Miller
Affiliation:
Keywords: Antiglioma activity, EDL-155 analogs, glioblastoma multiforme (GBM), tetrahydroisoquinoline (THI).
Abstract: Glioblastoma Multiforme (GBM) continues to demand improved chemotherapeutic solutions. In order to discover novel chemotherapeutic agents for GBM, we identified novel tetrahydroisoquinoline (THI) analogs as antiglioma agents. The present study reports the design, synthesis and in vitro evaluation of new THI derivatives in four established human glioma cell lines (T98, U87, LN18 and A172). Our structure activity relationship (SAR) studies revealed that the important modification of the carbon linker between the biphenyl and THI ring yielded EDL-360 (12) as a potent antiglioma agent (LN18; IC50: 5.42 ±0.06 μM) and is considered to be our new lead drug candidate for further preclinical studies.
Export Options
About this article
Cite this article as:
Patil Renukadevi, Hosni-Ahmed Amira, Jones S. Terreia, Patil A. Shivaputra, Asres B. Likeselam, Wang Xiangdi, Yates C. Ryan, Geisert E. Eldon and Miller D. Duane, Synthesis and In Vitro Evaluation of Novel 1,2,3,4-Tetrahydroisoquinoline Derivatives as Potent Antiglioma Agents, Anti-Cancer Agents in Medicinal Chemistry 2014; 14 (3) . https://dx.doi.org/10.2174/18715206113139990328
DOI https://dx.doi.org/10.2174/18715206113139990328 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
-
Microgravity Alters Cancer Growth and Progression
Current Cancer Drug Targets CDK Inhibitors: From the Bench to Clinical Trials
Current Drug Targets Molecular Imaging to Monitor Repair of Myocardial Infarction Using Genetically Engineered Bone Marrow-Derived Mesenchymal Stem Cells
Current Gene Therapy Insights into Ecto-5’-Nucleotidase as a New Target for Cancer Therapy: A Medicinal Chemistry Study
Current Medicinal Chemistry CETUXIMAB: From Bench to Bedside
Current Cancer Drug Targets In Vitro Synergistic Interaction between DTA0100 and Radiation in Human Cancer Cell Lines
Anti-Cancer Agents in Medicinal Chemistry NMR in Metabolic Profiles of Neural Stem/Progenitor Cells: Current Status and Relevant Problems
Current Medical Imaging Combination of Salinomycin and AZD3463 Reveals Synergistic Effect on Reducing the Viability of T98G Glioblastoma Cells
Anti-Cancer Agents in Medicinal Chemistry Nanosponge Carriers- An Archetype Swing in Cancer Therapy: A Comprehensive Review
Current Drug Targets Targeted Taxane Delivery Systems: Recent Advances
Drug Delivery Letters Editorial [ The Role of Epidermal Growth Factor Receptor (EGFR) Targeting Drugs in the Treatment of Cancer Guest Editor: Fortunato Ciardiello ]
Current Cancer Therapy Reviews Glutamine, Glucose and other Fuels for Cancer
Current Pharmaceutical Design Cell Metabolism Under Microenvironmental Low Oxygen Tension Levels in Stemness, Proliferation and Pluripotency
Current Molecular Medicine Bevacizumab and Angiogenesis Inhibitors in the Treatment of CNS Metastases: The Road less Travelled
Current Molecular Pharmacology A Novel Gene Selection Method Based on Sparse Representation and Max-Relevance and Min-Redundancy
Combinatorial Chemistry & High Throughput Screening High Throughput Screening for Colorectal Cancer Specific Compounds
Combinatorial Chemistry & High Throughput Screening Neurokinin-1 Receptor (NK-1R) Antagonists: Potential Targets in the Treatment of Glioblastoma Multiforme
Current Medicinal Chemistry Imidazoles and Benzimidazoles as Tubulin-Modulators for Anti-Cancer Therapy
Current Medicinal Chemistry MTHFR Gene Polymorphism and Diabetic Retinopathy
Current Diabetes Reviews Heparanase: Structure, Biological Functions, and Inhibition by Heparin-Derived Mimetics of Heparan Sulfate
Current Pharmaceutical Design