Abstract
Twenty-seven nitrated and non-nitrated compounds have been synthesized and tested for their growth inhibitory activity on three human cancer cells lines. Fourteen compounds were able to inhibit more than 50% of the growth of at least one of the cancer cell lines and five compounds exhibited high antiproliferative activity on human cancer cell lines (IC50 < 8.5 μM). The cytotoxicity of the compounds on Vero cell line was established in vitro to evaluate the selectivity. All active compounds have a good leaving group (bromide or chloride) at the benzylic position, indicating that the mechanism of action of these compounds is related to their alkylating properties. Two compounds (3 and 24) were selected for further studies in mice with Ehrlich solid tumors and display significant antitumor effects in vivo.
Keywords: Antitumor activity, alkylating agents, bioreduction, cytotoxicity, nitrocompounds, solid tumor.
Anti-Cancer Agents in Medicinal Chemistry
Title:Synthesis of Nitroaromatic Compounds as Potential Anticancer Agents
Volume: 15 Issue: 2
Author(s): Marcela Silva Lopes, Camila Filizzola de Andrade Sena, Bruno Leonardo Silva, Cristina Maria de Souza, Jonas Pereira Ramos, Geovanni Dantas Cassali, Elaine Maria de Souza-Fagundes, Ricardo Jose Alves, Mônica Cristina de Oliveira and Renata Barbosa de Oliveira
Affiliation:
Keywords: Antitumor activity, alkylating agents, bioreduction, cytotoxicity, nitrocompounds, solid tumor.
Abstract: Twenty-seven nitrated and non-nitrated compounds have been synthesized and tested for their growth inhibitory activity on three human cancer cells lines. Fourteen compounds were able to inhibit more than 50% of the growth of at least one of the cancer cell lines and five compounds exhibited high antiproliferative activity on human cancer cell lines (IC50 < 8.5 μM). The cytotoxicity of the compounds on Vero cell line was established in vitro to evaluate the selectivity. All active compounds have a good leaving group (bromide or chloride) at the benzylic position, indicating that the mechanism of action of these compounds is related to their alkylating properties. Two compounds (3 and 24) were selected for further studies in mice with Ehrlich solid tumors and display significant antitumor effects in vivo.
Export Options
About this article
Cite this article as:
Lopes Silva Marcela, de Andrade Sena Filizzola Camila, Silva Leonardo Bruno, de Souza Maria Cristina, Ramos Pereira Jonas, Cassali Dantas Geovanni, de Souza-Fagundes Maria Elaine, Alves Jose Ricardo, de Oliveira Cristina Mônica and de Oliveira Barbosa Renata, Synthesis of Nitroaromatic Compounds as Potential Anticancer Agents, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (2) . https://dx.doi.org/10.2174/1871520614666141114201749
DOI https://dx.doi.org/10.2174/1871520614666141114201749 |
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
-
Prevention and Treatment of Bone Metastases
Current Pharmaceutical Design ABC Transporters in Multidrug Resistance and Pharmacokinetics, and Strategies for Drug Development
Current Pharmaceutical Design New Targets of Therapy in T-Cell Lymphomas
Current Drug Targets Novel Aspects of Natural and Modified Vinca Alkaloids
Current Medicinal Chemistry - Anti-Cancer Agents Propofol Protects Against TNF-α-induced Blood-brain Barrier Disruption via the PIM-1/eNOS/NO Pathway
Current Neurovascular Research Metabolic Effects of Resveratrol in Mammals - a Link Between Improved Insulin Action and Aging
Current Aging Science Current Perspective of Natural Alkaloid Carbazole and its Derivatives as Antitumor Agents
Anti-Cancer Agents in Medicinal Chemistry MicroRNAs as Early Biomarkers in Obesity and Related Metabolic and Cardiovascular Diseases
Current Pharmaceutical Design Design of New Drug Molecules to be Used in Reversing Multidrug Resistance in Cancer Cells
Current Cancer Drug Targets Resistance of Cancer Cells to Targeted Therapies Through the Activation of Compensating Signaling Loops
Current Signal Transduction Therapy Nucleoside Transport as a Potential Target for Chemotherapy in Malaria
Current Pharmaceutical Design The Immunomodulatory Potential of Selected Bioactive Plant-Based Compounds in Breast Cancer: A Review
Anti-Cancer Agents in Medicinal Chemistry Deciphering Role of Cytokines for Therapeutic Strategies Against Rheumatoid Arthritis
Current Drug Targets The Development of Targeted Therapies for Hepatocellular Cancer
Current Pharmaceutical Design Myelodysplastic Syndromes: Review of Pathophysiology and Current Novel Treatment Approaches
Current Cancer Drug Targets Drugs, Environmental Factors, Loci and Genes Involved in Nonsyndromic Orofacial Cleft
Current Pharmacogenomics L1 Retrotransposon and Retinoblastoma: Molecular Linkages Between Epigenetics and Cancer
Current Molecular Medicine Anti-CD20 Antibody in Primary Sjogren's Syndrome Managemen
Current Pharmaceutical Biotechnology MicroRNAs as Cancer Biomarkers
MicroRNA Recent Progress on Antifungal Drug Development
Current Pharmaceutical Biotechnology