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Molecules
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Heterocyclic Compounds: Synthesis and Medicinal Chemistry Applications
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Heterocyclic Compounds: Synthesis and Medicinal Chemistry Applications

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 31 May 2024 | Viewed by 3242

Special Issue Editors

Prof. Dr. Maria Novella Romanelli

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Guest Editor
Department of Neuroscience, Psychology, Drug Research and Child’s Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy
Interests: enzyme modulators; ion channel modulators; multi-target ligands; antihyperalgesic agents; receptor modulators
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Silvia Dei

E-Mail Website
Guest Editor
Department of Neuroscience, Psychology, Drug Research and Child’s Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy
Interests: anticancer drugs; PGP modulators; antibacterials; multitarget-ligands; receptor modulators
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

According to several statistical analyses, a high percentage of drugs or biologically-active compounds contain aliphatic or aromatic heterocycles. Such moieties can be an essential part of the pharmacophore (antifungal azoles are an example) or may be used to modify ADME/TOX properties (for instance, piperazines in kinase inhibitors). Heterocycles can be used in drug design following optimization strategies such as bioisosterism or scaffold-hopping; in particular, nitrogen-containing heterocycles can be introduced to provide basic or H-bond forming groups to improve both the pharmacological and pharmaceutical profiles of the drug candidate. Owing to such wide application, the published synthetic methods are continuously applied and optimized to obtain new derivatives, and new synthetic methods are constantly developed in order to overcome the limitations of the existing procedures. In recent times, it has been also possible to obtain heterocycles containing elements largely ignored in medicinal chemistry such as silicon, selenium, phosphorous or boron, and, in some cases, to obtain drugs, such as vaborbactam, a beta-lactamase inhibitor that has been approved for therapy.

Prof. Dr. Maria Novella Romanelli
Prof. Dr. Silvia Dei
Guest Editors

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. Molecules 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 2700 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

  • medicinal chemistry
  • heterocycles
  • organic synthesis
  • natural products
  • pharmacophore
  • artificial intelligence
  • CNS drugs
  • antibacterial agents
  • antiviral drugs
  • anticancer agents
  • enzyme modulators
  • receptor modulators
  • ion channel modulators

Published Papers (2 papers)

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Review

24 pages, 11879 KiB  
Review
Insights on Antitumor Activity and Mechanism of Natural Benzophenanthridine Alkaloids
by Rui Peng, Mengwei Xu, Baocheng Xie, Qing Min, Siwen Hui, Ziwei Du, Yan Liu, Wei Yu, Shi Wang, Xin Chen, Guang Yang, Zhaofang Bai, Xiaohe Xiao and Shuanglin Qin
Molecules 2023, 28(18), 6588; https://doi.org/10.3390/molecules28186588 - 13 Sep 2023
Cited by 1 | Viewed by 1635
Abstract
Benzophenanthridine alkaloids are a class of isoquinoline compounds, which are widely found in the plants of papaveraceae, corydalis, and rutaceae. Biological activities and clinical studies have shown that benzophenanthridine alkaloids have inhibitory effects on many cancers. Considering that the anticancer [...] Read more.
Benzophenanthridine alkaloids are a class of isoquinoline compounds, which are widely found in the plants of papaveraceae, corydalis, and rutaceae. Biological activities and clinical studies have shown that benzophenanthridine alkaloids have inhibitory effects on many cancers. Considering that the anticancer activities and mechanisms of many natural benzophenanthridine alkaloids have been discovered in succession, the purpose of this paper is to review the anticancer effects of benzophenanthridine alkaloids and explore the application potential of these natural products in the development of antitumor drugs. A literature survey was carried out using Scopus, Pubmed, Reaxys, and Google Scholar databases. This review summarizes and analyzes the current status of research on the antitumor activity and antitumor mechanism of natural products of benzophenanthridine from different sources. The research progress of the antitumor activity of natural products of benzophenanthridine from 1983 to 2023 was reviewed. The antitumor activities of 90 natural products of benzophenanthridine and their related analogues were summarized, and the results directly or indirectly showed that natural products of benzophenanthridine had the effects of antidrug-resistant tumor cell lines, antitumor stem cells, and inducing ferroptosis. In conclusion, benzophenanthridine alkaloids have inhibitory effects on a variety of cancers and have the potential to counteract tumor resistance, and they have great application potential in the development of antitumor drugs. Full article
(This article belongs to the Special Issue Heterocyclic Compounds: Synthesis and Medicinal Chemistry Applications)
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33 pages, 4554 KiB  
Review
Nortopsentins as Leads from Marine Organisms for Anticancer and Anti-Inflammatory Agent Development
by Camilla Pecoraro, Francesca Terrana, Giovanna Panzeca, Barbara Parrino, Stella Cascioferro, Patrizia Diana, Elisa Giovannetti and Daniela Carbone
Molecules 2023, 28(18), 6450; https://doi.org/10.3390/molecules28186450 - 05 Sep 2023
Cited by 2 | Viewed by 1276
Abstract
The marine environment is an excellent source of molecules that have a wide structural diversity and a variety of biological activities. Many marine natural products (MNPs) have been established as leads for anticancer drug discovery. Most of these compounds are alkaloids, including several [...] Read more.
The marine environment is an excellent source of molecules that have a wide structural diversity and a variety of biological activities. Many marine natural products (MNPs) have been established as leads for anticancer drug discovery. Most of these compounds are alkaloids, including several chemical subclasses. In this review, we focus on the bis-indolyl alkaloid Nortopsentins and their derivatives with antiproliferative properties. Nortopsentins A–C were found to exhibit in vitro cytotoxicity against the P388 murine leukaemia cell line. Their structural manipulation provided a wide range of derivatives with significant anti-tumour activity against human cell lines derived from different cancer types (bladder, colon, gastric, CNS, liver, lung, breast, melanoma, ovarian, pancreatic, prostate, pleural mesothelioma, renal, sarcoma, and uterus). In vivo assays on animal models also proved that Nortopsentins and related bis-indolyl compounds have potent anti-inflammatory activity. These remarks set the foundation for future investigations into the development of new Nortopsentin derivatives as new anticancer and anti-inflammatory agents. Full article
(This article belongs to the Special Issue Heterocyclic Compounds: Synthesis and Medicinal Chemistry Applications)
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