Abstract
A large group of aminoalkyl and aminoalkanol derivatives of selected dicarboximides were synthesized and characterized by 1HNMR, 13CNMR and ESI MS spectra analysis. The thirty nine new compounds were tested for their cytotoxic properties in human chronic (K562), acute leukemia (HL-60), and cervical cancer cells (HeLa) as well as in normal endothelial cells (HUVEC). The most promising compounds are 4-[2-(dimethylamino)ethyl]-, (diethylamino) ethyl]-, 4-[2-(piperidin-1-yl)ethyl]-, 4-[3-(dimethylamino)propyl]- and 4-[2-hydroxy-3-(propan- 2-ylamino)propyl]- derivatives of 1,7-diethyl-8,9-diphenyl-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5,10-trione exhibiting high and selective cytotoxicity towards K562 and HL-60 cells (IC50 in the range of 1-10 µM) while being non-toxic towards HUVEC and HeLa cells (IC50> 100 μM). Moreover, the preliminary studies have showed that 4-[2-(piperidin-1-yl)ethyl]- 1,7-diethyl-8,9-diphenyl-4-azatricyclo [5.2.1.02,6]dec-8-ene-3,5,10-trione induces programmed cell death (apoptosis) in leukemia cells.
Keywords: Dicarboximides, cytotoxic properties, HeLa, HL-60, K562, apoptosis.
Graphical Abstract
Anti-Cancer Agents in Medicinal Chemistry
Title:New, Substituted Derivatives of Dicarboximides and their Cytotoxic Properties
Volume: 16 Issue: 7
Author(s): Bożena Kuran, Mariola Napiórkowska, Jerzy Kossakowski, Marcin Cieślak, Julia Kaźmierczak-Barańska, Karolina Królewska and Barbara Nawrot
Affiliation:
Keywords: Dicarboximides, cytotoxic properties, HeLa, HL-60, K562, apoptosis.
Abstract: A large group of aminoalkyl and aminoalkanol derivatives of selected dicarboximides were synthesized and characterized by 1HNMR, 13CNMR and ESI MS spectra analysis. The thirty nine new compounds were tested for their cytotoxic properties in human chronic (K562), acute leukemia (HL-60), and cervical cancer cells (HeLa) as well as in normal endothelial cells (HUVEC). The most promising compounds are 4-[2-(dimethylamino)ethyl]-, (diethylamino) ethyl]-, 4-[2-(piperidin-1-yl)ethyl]-, 4-[3-(dimethylamino)propyl]- and 4-[2-hydroxy-3-(propan- 2-ylamino)propyl]- derivatives of 1,7-diethyl-8,9-diphenyl-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5,10-trione exhibiting high and selective cytotoxicity towards K562 and HL-60 cells (IC50 in the range of 1-10 µM) while being non-toxic towards HUVEC and HeLa cells (IC50> 100 μM). Moreover, the preliminary studies have showed that 4-[2-(piperidin-1-yl)ethyl]- 1,7-diethyl-8,9-diphenyl-4-azatricyclo [5.2.1.02,6]dec-8-ene-3,5,10-trione induces programmed cell death (apoptosis) in leukemia cells.
Export Options
About this article
Cite this article as:
Kuran Bożena, Napiórkowska Mariola, Kossakowski Jerzy, Cieślak Marcin, Kaźmierczak-Barańska Julia, Królewska Karolina and Nawrot Barbara, New, Substituted Derivatives of Dicarboximides and their Cytotoxic Properties, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (7) . https://dx.doi.org/10.2174/1871520616666160223114318
DOI https://dx.doi.org/10.2174/1871520616666160223114318 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |

- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
-
Idronoxil as an Anticancer Agent: Activity and Mechanisms
Current Cancer Drug Targets Protein-Protein Interactions: Recent Progress in the Development of Selective PDZ Inhibitors
Current Chemical Biology Mesenchymal Cells in the Treatment of Spinal Cord Injury: Current & Future Perspectives
Current Stem Cell Research & Therapy Copper Complexes as Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Radiopharmaceuticals in Tumor Hypoxia Imaging: A Review Focused on Medicinal Chemistry Aspects
Anti-Cancer Agents in Medicinal Chemistry Recent Developments in the Field of Tumor-Inhibiting Metal Complexes
Current Pharmaceutical Design Protein Kinase C ζ Drives Sphingomyelin Metabolism in the Nucleus During Cell Proliferation
Current Chemical Biology The Effects of Curcumin on Immune Responses
Current Bioactive Compounds Photodynamic Effects of Vitamin K3 on Cervical Carcinoma Cells Activating Mitochondrial Apoptosis Pathways
Anti-Cancer Agents in Medicinal Chemistry Gene Therapy and Cell Reprogramming For the Aging Brain: Achievements and Promise
Current Gene Therapy Neoisoliquiritigenin Inhibits Tumor Progression by Targeting GRP78-β- catenin Signaling in Breast Cancer
Current Cancer Drug Targets Th17 and Treg Cells, Two New Lymphocyte Subpopulations with a Key Role in the Immune Response Against Infection
Infectious Disorders - Drug Targets Recent Advances for the Synthesis of Selenium-containing Small Molecules as Potent Antitumor Agents
Current Medicinal Chemistry The Clinical Perspective on Value of 3D, Thin Slice T2-Weighted Images in 3T Pelvic MRI for Tumors
Current Medical Imaging Overview of Base Excision Repair Biochemistry
Current Molecular Pharmacology Histopathology, Immunohistochemistry and Molecular Biology of Follicular Epithelium-Derived Pediatric Thyroid Carcinomas
Current Pediatric Reviews Intranasal Fluorescent Nanocrystals for Longitudinal <i>In Vivo</i> Evaluation of Cerebral Microlesions
Pharmaceutical Nanotechnology Long Non-coding RNA AFAP1-AS1 Facilitates Prostate Cancer Progression by Regulating miR-15b/IGF1R Axis
Current Pharmaceutical Design Genetic Variations in Telomere Maintenance, with Implications on Tissue Renewal Capacity and Chronic Disease Pathologies
Current Pharmacogenomics and Personalized Medicine Repurposing Chloroquine Analogs as an Adjuvant Cancer Therapy
Recent Patents on Anti-Cancer Drug Discovery