Special Issue "Recent Developments in the Medicinal Chemistry of Pyrroles"

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 30 September 2021.

Special Issue Editor

Dr. Antonella Messore
E-Mail Website
Guest Editor
Department of Pharmaceutical Chemistry and drug Technology "Sapienza" University of Rome, Rome, Italy
Interests: drug design; synthesis of new potential bioactive compounds in the field of anticancer, antiviral and antiparasitic agents; structure–activity relationship study; organic synthesis

Special Issue Information

Dear Colleagues,

Pyrrole is a heterocyclic ring widespread in biologically active natural products and synthetic molecules. Pyrrole-based compounds exhibit a wide spectrum of bioactivity making such heterocyclic core a privileged scaffold and a versatile pharmacophore in medicinal chemistry. Due to their biological potential, pyrroles have gained great attention and they have been successfully used in the development of new derivatives. Some drugs containing pyrrole moiety are already available on the market while the rest are under clinical trials.

In this Special Issue, authors are invited to submit original research articles, reviews, and short communications exploring recent advances in pyrrole-based medicinal chemistry. Topics of interest include but are not limited to antiviral, anticancer, antiprotozoal, antitubercular, antioxidant, and enzyme inhibiting activities.

Dr. Antonella Messore
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 papers will be 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. Pharmaceuticals is an international peer-reviewed open access monthly 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 1800 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

  • pyrrole heterocycles
  • N-substituted pyrrole
  • natural pyrrole derivatives
  • synthetic pyrroles
  • bioactive pyrroles.

Published Papers (2 papers)

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Research

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Article
Anti-Tumoral Effects of a (1H-Pyrrol-1-yl)Methyl-1H-Benzoimidazole Carbamate Ester Derivative on Head and Neck Squamous Carcinoma Cell Lines
Pharmaceuticals 2021, 14(6), 564; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14060564 - 12 Jun 2021
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Abstract
Nocodazole is an antineoplastic agent that exerts its effects by depolymerizing microtubules. Herein we report a structural analog of nocodazole, a (1H-pyrrol-1-yl)methyl-1H-benzoimidazole carbamate ester derivative, named RDS 60. We evaluated the antineoplastic properties of RDS 60 in two human [...] Read more.
Nocodazole is an antineoplastic agent that exerts its effects by depolymerizing microtubules. Herein we report a structural analog of nocodazole, a (1H-pyrrol-1-yl)methyl-1H-benzoimidazole carbamate ester derivative, named RDS 60. We evaluated the antineoplastic properties of RDS 60 in two human head and neck squamous cell carcinoma (HNSCC) cell lines and we found that this compound significantly inhibited replication of both HNSCC cell lines without inducing any important cytotoxic effect on human dermal fibroblasts and human keratinocytes. The treatment of HNSCC cell lines with 1 μM RDS 60 for 24 h stopped development of normal bipolar mitotic spindles and, at the same time, blocked the cell cycle in G2/M phase together with cytoplasmic accumulation of cyclin B1. Consequently, treatment with 2 μM RDS 60 for 24 h induced the activation of apoptosis in both HNSCC cell lines. Additionally, RDS 60 was able to reverse the epithelial-mesenchymal transition and to inhibit cell migration and extracellular matrix infiltration of both HNSCC cell lines. The reported results demonstrate that this compound has a potent effect in blocking cell cycle, inducing apoptosis and inhibiting cell motility and stromal invasion of HNSCC cell lines. Therefore, the ability of RDS 60 to attenuate the malignancy of tumor cells suggests its potential role as an interesting and powerful tool for new approaches in treating HNSCC. Full article
(This article belongs to the Special Issue Recent Developments in the Medicinal Chemistry of Pyrroles)
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Review

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Review
An Overview of the Biological Activity of Pyrrolo[3,4-c]pyridine Derivatives
Pharmaceuticals 2021, 14(4), 354; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14040354 - 11 Apr 2021
Cited by 2 | Viewed by 561
Abstract
Pyrrolo[3,4-c]pyridine is one of the six structural isomers of the bicyclic ring system containing a pyrrole moiety fused to a pyridine nucleus. The broad spectrum of pharmacological properties of pyrrolo[3,4-c]pyridine derivatives is the main reason for developing new compounds [...] Read more.
Pyrrolo[3,4-c]pyridine is one of the six structural isomers of the bicyclic ring system containing a pyrrole moiety fused to a pyridine nucleus. The broad spectrum of pharmacological properties of pyrrolo[3,4-c]pyridine derivatives is the main reason for developing new compounds containing this scaffold. This review presents studies on the biological activity of pyrrolo[3,4-c]pyridines that have been reported in the scientific literature. Most of these derivatives have been studied as analgesic and sedative agents. Biological investigations have shown that pyrrolo[3,4-c]pyridines can be used to treat diseases of the nervous and immune systems. Their antidiabetic, antimycobacterial, antiviral, and antitumor activities also have been found. Full article
(This article belongs to the Special Issue Recent Developments in the Medicinal Chemistry of Pyrroles)
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