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Applied Sciences
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Carbazole Derivatives: Latest Advances and Prospects
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Carbazole Derivatives: Latest Advances and Prospects

A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Applied Biosciences and Bioengineering".

Deadline for manuscript submissions: closed (20 August 2022) | Viewed by 13420

Printed Edition Available!
A printed edition of this Special Issue is available here.

Special Issue Editor

Dr. Anna Caruso

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Guest Editor
Department of Pharmacy, Health & Nutritional Sciences, University of Calabria, 87036 Arcavacata, Italy
Interests: carbazole derivatives; heterocyclic compounds synthesis; antioxidants; medicinal chemistry; medicinal compounds synthesis
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In recent years, plenty of research has been aimed at the multiple properties of different carbazole derivatives. Carbazoles are important aromatic heterocyclic compounds isolated from plants, such as those of the genera Ochrosia, Murraya, Glycosmis, and Clausena, or synthetically obtained.

Today, many carbazole derivatives are widely studied as photoconductive, anti-bacterial, anti-fungal, anticancer, antioxidant, anti-inflammatory, anti-Alzheimer, anti-malarial, anti-tuberculosis, and anti-viral agents, for the treatment of obesity and for their psychotropic and anti-histamine activities. However, the therapeutic applications and benefits of some of these derivatives remain low because of their low hydrosolubility, low bioavailability, and the onset of some side effects.

For these reasons, the purpose of this Special Issue "Carbazole Derivatives: Latest Advances and Prospects" is to report the molecular modeling, synthesis, and biological evaluation of new carbazole derivatives with improved pharmacokinetic and pharmacodinamic properties for their development in medicinal chemistry.

Dr. Anna Caruso
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Applied Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2400 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • carbazole derivatives
  • medicinal chemistry
  • drug development
  • heterocyclic compounds
  • biological properties
  • docking simulation
  • enhanced cellular uptake
  • innovative vehicles

Published Papers (6 papers)

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Editorial

Jump to: Research, Review

2 pages, 163 KiB  
Editorial
Special Issue “Carbazole Derivatives: Latest Advances and Prospects”
by Anna Caruso
Appl. Sci. 2023, 13(7), 4263; https://0-doi-org.brum.beds.ac.uk/10.3390/app13074263 - 28 Mar 2023
Cited by 1 | Viewed by 861
Abstract
The academic community has extensively explored, over the years, heterocyclic compounds of the carbazolic motif [...] Full article
(This article belongs to the Special Issue Carbazole Derivatives: Latest Advances and Prospects)

Research

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12 pages, 2280 KiB  
Article
A Nitrocarbazole as a New Microtubule-Targeting Agent in Breast Cancer Treatment
by Maria Stefania Sinicropi, Cinzia Tavani, Camillo Rosano, Jessica Ceramella, Domenico Iacopetta, Alexia Barbarossa, Lara Bianchi, Alice Benzi, Massimo Maccagno, Marco Ponassi, Domenico Spinelli and Giovanni Petrillo
Appl. Sci. 2021, 11(19), 9139; https://doi.org/10.3390/app11199139 - 01 Oct 2021
Cited by 7 | Viewed by 2019
Abstract
Breast cancer is still considered a high-incidence disease, and numerous are the research efforts for the development of new useful and effective therapies. Among anticancer drugs, carbazole compounds are largely studied for their anticancer properties and their ability to interfere with specific targets, [...] Read more.
Breast cancer is still considered a high-incidence disease, and numerous are the research efforts for the development of new useful and effective therapies. Among anticancer drugs, carbazole compounds are largely studied for their anticancer properties and their ability to interfere with specific targets, such as microtubule components. The latter are involved in vital cellular functions, and the perturbation of their dynamics leads to cell cycle arrest and subsequent apoptosis. In this context, we report the anticancer activity of a series of carbazole analogues 1–8. Among them, 2-nitrocarbazole 1 exhibited the best cytotoxic profile, showing good anticancer activity against two breast cancer cell lines, namely MCF-7 and MDA-MB-231, with IC50 values of 7 ± 1.0 and 11.6 ± 0.8 μM, respectively. Furthermore, compound 1 did not interfere with the growth of the normal cell line MCF-10A, contrarily to Ellipticine, a well-known carbazole derivative used as a reference molecule. Finally, in vitro immunofluorescence analysis and in silico studies allowed us to demonstrate the ability of compound 1 to interfere with tubulin organization, similarly to vinblastine: a feature that results in triggering MCF-7 cell death by apoptosis, as demonstrated using a TUNEL assay. Full article
(This article belongs to the Special Issue Carbazole Derivatives: Latest Advances and Prospects)
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16 pages, 2950 KiB  
Article
Carbazole and Simplified Derivatives: Novel Tools toward β-Adrenergic Receptors Targeting
by Fedora Grande, Anna De Bartolo, Maria Antonietta Occhiuzzi, Anna Caruso, Carmine Rocca, Teresa Pasqua, Alessia Carocci, Vittoria Rago, Tommaso Angelone and Maria Stefania Sinicropi
Appl. Sci. 2021, 11(12), 5486; https://0-doi-org.brum.beds.ac.uk/10.3390/app11125486 - 13 Jun 2021
Cited by 7 | Viewed by 1962
Abstract
β-Adrenergic receptors (β-ARs) are G protein-coupled receptors involved in important physiological and pathological processes related to blood pressure and cardiac activity. The inhibition of cardiac β1-ARs could be beneficial in myocardial hypertrophy, ischemia and failure. Several carbazole-based compounds have [...] Read more.
β-Adrenergic receptors (β-ARs) are G protein-coupled receptors involved in important physiological and pathological processes related to blood pressure and cardiac activity. The inhibition of cardiac β1-ARs could be beneficial in myocardial hypertrophy, ischemia and failure. Several carbazole-based compounds have been described as promising β-blockers. Herein, we investigate the capability of a carbazole derivative and three simplified indole analogs to interact with the active binding site of β1-AR by molecular docking studies. In the light of the obtained results, our compounds were tested by biological assays in H9c2 cardiomyocytes exposed to isoproterenol (ISO) to confirm their potential as β1-blockers agents, and two of them (8 and 10) showed interesting and promising properties. In particular, these compounds were effective against ISO-dependent in vitro cardiac hypertrophy, even at concentrations lower than the known β-AR antagonist propranolol. Overall, the data suggest that the indole derivatives 8 and 10 could act as potent β1-blockers and, active at low doses, could elicit limited side effects. Full article
(This article belongs to the Special Issue Carbazole Derivatives: Latest Advances and Prospects)
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Review

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15 pages, 3127 KiB  
Review
An Update of Carbazole Treatment Strategies for COVID-19 Infection
by Maria Grazia Bonomo, Anna Caruso, Hussein El-Kashef, Giovanni Salzano, Maria Stefania Sinicropi and Carmela Saturnino
Appl. Sci. 2023, 13(3), 1522; https://0-doi-org.brum.beds.ac.uk/10.3390/app13031522 - 24 Jan 2023
Cited by 3 | Viewed by 1984
Abstract
The Coronavirus disease 2019 (COVID-19) outbreak was declared by the World Health Organization (WHO) in March 2020 to be a pandemic and many drugs used at the beginning proved useless in fighting the infection. Lately, there has been approval of some new generation [...] Read more.
The Coronavirus disease 2019 (COVID-19) outbreak was declared by the World Health Organization (WHO) in March 2020 to be a pandemic and many drugs used at the beginning proved useless in fighting the infection. Lately, there has been approval of some new generation drugs for the clinical treatment of severe or critical COVID-19 infections. Nevertheless, more drugs are required to reduce the pandemic’s impact. Several treatment approaches for COVID-19 were employed since the beginning of the pandemic, such as immunomodulatory, antiviral, anti-inflammatory, antimicrobial agents, and again corticosteroids, angiotensin II receptor blockers, and bradykinin B2 receptor antagonists, but many of them were proven ineffective in targeting the virus. So, the identification of drugs to be used effectively for treatment of COVID-19 is strongly needed. It is aimed in this review to collect the information so far known about the COVID-19 studies and treatments. Moreover, the observations reported in this review about carbazoles as a treatment can signify a potentially useful clinical application; various drugs that can be introduced into the therapeutic equipment to fight COVID-19 or their molecules can be used as the basis for designing new antivirals. Full article
(This article belongs to the Special Issue Carbazole Derivatives: Latest Advances and Prospects)
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17 pages, 3850 KiB  
Review
Carbazoles: Role and Functions in Fighting Diabetes
by Fedora Grande, Giuseppina Ioele, Anna Caruso, Maria Antonietta Occhiuzzi, Hussein El-Kashef, Carmela Saturnino and Maria Stefania Sinicropi
Appl. Sci. 2023, 13(1), 349; https://0-doi-org.brum.beds.ac.uk/10.3390/app13010349 - 27 Dec 2022
Cited by 4 | Viewed by 1950
Abstract
Carbazole derivatives have gained a lot of attention in medicinal chemistry over the last few decades due to their wide range of biological and pharmacological properties, including antibacterial, antitumor, antioxidant, and anti-inflammatory activities. The therapeutic potential of natural, semi-synthetic or synthetic carbazole-containing molecules [...] Read more.
Carbazole derivatives have gained a lot of attention in medicinal chemistry over the last few decades due to their wide range of biological and pharmacological properties, including antibacterial, antitumor, antioxidant, and anti-inflammatory activities. The therapeutic potential of natural, semi-synthetic or synthetic carbazole-containing molecules has expanded considerably owing to their role in the pathogenesis and development of diabetes. Several studies have demonstrated the ability of carbazole derivatives to reduce oxidative stress, block adrenergic hyperactivation, prevent damage to pancreatic cells and modulate carbohydrate metabolism. In this survey, we summarize the latest advances in the synthetic and natural carbazole-containing compounds involved in diabetes pathways. Full article
(This article belongs to the Special Issue Carbazole Derivatives: Latest Advances and Prospects)
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26 pages, 12918 KiB  
Review
Carbazole Derivatives as STAT Inhibitors: An Overview
by Anna Caruso, Alexia Barbarossa, Alessia Carocci, Giovanni Salzano, Maria Stefania Sinicropi and Carmela Saturnino
Appl. Sci. 2021, 11(13), 6192; https://0-doi-org.brum.beds.ac.uk/10.3390/app11136192 - 03 Jul 2021
Cited by 11 | Viewed by 2949
Abstract
The carbazole class is made up of heterocyclically structured compounds first isolated from coal tar. Their structural motif is preponderant in different synthetic materials and naturally occurring alkaloids extracted from the taxonomically related higher plants of the genus Murraya, Glycosmis, and [...] Read more.
The carbazole class is made up of heterocyclically structured compounds first isolated from coal tar. Their structural motif is preponderant in different synthetic materials and naturally occurring alkaloids extracted from the taxonomically related higher plants of the genus Murraya, Glycosmis, and Clausena from the Rutaceae family. Concerning the biological activity of these compounds, many research groups have assessed their antiproliferative action of carbazoles on different types of tumoral cells, such as breast, cervical, ovarian, hepatic, oral cavity, and small-cell lung cancer, and underlined their potential effects against psoriasis. One of the principal mechanisms likely involved in these effects is the ability of carbazoles to target the JAK/STATs pathway, considered essential for cell differentiation, proliferation, development, apoptosis, and inflammation. In this review, we report the studies carried out, over the years, useful to synthesize compounds with carbazole moiety designed to target these kinds of kinases. Full article
(This article belongs to the Special Issue Carbazole Derivatives: Latest Advances and Prospects)
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