Abstract
Chemotherapeutics used in cancer treatment may elicit pleiotropic effects interfering, for instance, directly on DNA metabolism or on endoplasmic organelles functions. Recently there has been a trend towards the use of molecular-targeted therapies as alternative treatments of cancer, arising from the need to overcome the onset of undesired side effects or drug-resistance. Thus, a major challenge is the design and synthesis of new agents able to interact with specific cellular components, often over-expressed or altered in cancerous cells, such as telomerase and topoisomerase or protein kinases, with reduced toxicity at effective doses. The main molecular targets for the development of new anticancer drugs include: cell surface receptors, signal transduction pathways, enzymes, gene transcription, ubiquitin-proteasome/heat shock proteins, and anti-angiogenic agents. Several natural or synthetic polycyclic molecules with carbazolic nucleus, which show attractive drug-like properties, were identified with the aim to increase their biological activities and their specificity, obtaining cytotoxic agents effective in a panel of cancer cell lines. The cytotoxic profile of these compounds has been assessed using several in vitro assays as, for instance, MTT, colony formation, and flow cytometry assays and some of these compounds showed an interesting profile at sub-micromolar concentrations. The usefulness of some carbazole derivatives has been demonstrated, as well, in preclinical studies.
Keywords: Anticancer drugs, alkaloids, breast cancer, carbazole derivatives, ellipticine, polycyclic compounds.
Mini-Reviews in Medicinal Chemistry
Title:Carbazole derivatives: a promising scenario for breast cancer treatment
Volume: 16 Issue: 8
Author(s): Anna Caruso, Domenico Iacopetta, Francesco Puoci, Anna Rita Cappello, Carmela Saturnino and Maria Stefania Sinicropi
Affiliation:
Keywords: Anticancer drugs, alkaloids, breast cancer, carbazole derivatives, ellipticine, polycyclic compounds.
Abstract: Chemotherapeutics used in cancer treatment may elicit pleiotropic effects interfering, for instance, directly on DNA metabolism or on endoplasmic organelles functions. Recently there has been a trend towards the use of molecular-targeted therapies as alternative treatments of cancer, arising from the need to overcome the onset of undesired side effects or drug-resistance. Thus, a major challenge is the design and synthesis of new agents able to interact with specific cellular components, often over-expressed or altered in cancerous cells, such as telomerase and topoisomerase or protein kinases, with reduced toxicity at effective doses. The main molecular targets for the development of new anticancer drugs include: cell surface receptors, signal transduction pathways, enzymes, gene transcription, ubiquitin-proteasome/heat shock proteins, and anti-angiogenic agents. Several natural or synthetic polycyclic molecules with carbazolic nucleus, which show attractive drug-like properties, were identified with the aim to increase their biological activities and their specificity, obtaining cytotoxic agents effective in a panel of cancer cell lines. The cytotoxic profile of these compounds has been assessed using several in vitro assays as, for instance, MTT, colony formation, and flow cytometry assays and some of these compounds showed an interesting profile at sub-micromolar concentrations. The usefulness of some carbazole derivatives has been demonstrated, as well, in preclinical studies.
Export Options
About this article
Cite this article as:
Caruso Anna, Iacopetta Domenico, Puoci Francesco, Cappello Rita Anna, Saturnino Carmela and Sinicropi Stefania Maria, Carbazole derivatives: a promising scenario for breast cancer treatment, Mini-Reviews in Medicinal Chemistry 2016; 16 (8) . https://dx.doi.org/10.2174/1389557515666150709111342
DOI https://dx.doi.org/10.2174/1389557515666150709111342 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Drugs and mitochondria
Mitochondria play a central role in the life and death of cells. They are not merely the center for energy metabolism but are also the headquarters for different catabolic and anabolic processes, calcium fluxes, and various signaling pathways. Mitochondria maintain homeostasis in the cell by interacting with reactive oxygen-nitrogen species ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer’s, Parkinson’s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...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
-
Targeted Drug Delivery: Trends and Perspectives
Current Drug Delivery 1,3,4-Thiadiazole Based Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Drug Transport Across the Blood-Brain Barrier and the Impact of Breast Cancer Resistance Protein (ABCG2)
Current Topics in Medicinal Chemistry Targeting Negative Regulators of TRIF-dependent TLR Signaling Pathway as a Novel Therapeutic Strategy
Current Signal Transduction Therapy Medicinal Plants as a Source of New Therapeutic Products: Genus Mentha and the Potential Antimicrobial Activity of Extracts and Essential Oils
Current Traditional Medicine The Application of Fungal Beta-glucans for the Treatment of Colon Cancer
Anti-Cancer Agents in Medicinal Chemistry Tobacco, Inflammation, and Respiratory Tract Cancer
Current Pharmaceutical Design <i>Circular RNA NF1-419</i> Inhibits Proliferation and Induces Apoptosis by Regulating Lipid Metabolism in Astroglioma Cells
Recent Patents on Anti-Cancer Drug Discovery Overview of Inorganic Nanoparticles: An Expanding Horizon in Tumor Therapeutics
Recent Patents on Anti-Cancer Drug Discovery Extensive Computational Studies for the Identification of Potential Therapeutic Candidates Against Breast Cancer
Current Indian Science The Role of Mediterranean Diet, CoQ10 and Conjugated-Melatonin in Osteoporosis Primary Prevention and Therapy
Current Nutrition & Food Science TRYCAT Pathways Link Peripheral Inflammation, Nicotine, Somatization and Depression in the Etiology and Course of Parkinson’s Disease
CNS & Neurological Disorders - Drug Targets Stochastic Neighbor Embedding Algorithm and its Application in Molecular Biological Data
Current Bioinformatics Surface Markers of Cancer Stem Cells in Solid Tumors
Current Stem Cell Research & Therapy A Comprehensive Review on Pharmacology and Toxicology of Bioactive Compounds of <i>Lagerstroemia Speciosa(L.</i>) Pers.
Current Traditional Medicine Intercalators as Anticancer Drugs
Current Pharmaceutical Design Signaling Molecules: The Pathogenic Role of the IL-6/STAT-3 Trans Signaling Pathway in Intestinal Inflammation and in Colonic Cancer
Current Drug Targets Effects of Tea Polyphenols and their Polymers on MAPK Signaling Pathways in Cancer Research
Mini-Reviews in Medicinal Chemistry Frontline Management of Advanced Epithelial Ovarian Cancer: A Comprehensive Statement by the Africa Middle East Cancer Inter-group [AMCI]
Current Women`s Health Reviews Preface
Current Radiopharmaceuticals