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Heterocyclic Compounds: Design, Synthesis, and Applications

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

Deadline for manuscript submissions: closed (31 December 2021) | Viewed by 6559

Special Issue Editor


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Guest Editor
Dipartimento di Scienza e Alta Tecnologia, Università degli Studi dell'Insubria, via Valleggio 9, 22100 Como, Italy
Interests: organic synthesis; indoles; biindole compounds, natural products; nitrosoarenes; alkynes; bioactive compounds; annulations; cycloaddition, material science
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Special Issue Information

Dear Colleagues,

In the almost two hundred years of history of synthetic organic chemistry (starting from the milestone of the Wohler’s preparation of urea in 1828), heterocycles have occupied an ever-growing space both in the research of academia and industry. Novel methodologies of preparations and novel characteristics of heterocyclic products are frequently and regularly developed every day.

Heterocyclic compounds play a fundamental role in everyday life and are the most diffuse category of organic molecules that are known as useful intermediates, interesting scaffolds, relevant building blocks, and highly valuable fine chemicals extensively used in medicinal chemistry as well as in material science. Research on API (active pharmaceutical ingredients) is particularly involved and connected with the preparation of novel heterocyclic compounds that are suitable for different screening in innovative kinds of therapies for many diseases. Heterocycles are even diffused in the new materials that are continuously discovered with peculiar features and utilities as semiconductors, sensors, or any other role in the interdisciplinary field of material science. Many future devices that are going to be used soon are strongly linked and associated with heterocyclic compounds. Biochemistry is another field in which heterocycles show a ubiquitous role and there is probably no biochemical pathway without heterocyclic molecules. This Special Issue aims to show the multiplicity of actions that heterocycles play, representing an enormous class of products. I have the privilege and honor to serve as Guest Editor for this Special Issue of Molecules on “Heterocyclic Compounds: Design, Synthesis, and Applications”. I would thus like to invite all those who are involved in heterocyclic chemistry to participate and contribute to this issue.

Prof. Dr. Andrea Penoni
Guest Editor

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Keywords

  • cyclization
  • heterocycles
  • bioactive compounds
  • medicinal chemistry
  • natural products
  • annulations
  • material science
  • building blocks
  • fine chemicals

Published Papers (2 papers)

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Research

17 pages, 23490 KiB  
Article
Exploring the Synergistic Anticancer Potential of Benzofuran–Oxadiazoles and Triazoles: Improved Ultrasound- and Microwave-Assisted Synthesis, Molecular Docking, Hemolytic, Thrombolytic and Anticancer Evaluation of Furan-Based Molecules
by Ali Irfan, Sadia Faiz, Azhar Rasul, Rehman Zafar, Ameer Fawad Zahoor, Katarzyna Kotwica-Mojzych and Mariusz Mojzych
Molecules 2022, 27(3), 1023; https://doi.org/10.3390/molecules27031023 - 02 Feb 2022
Cited by 14 | Viewed by 2474
Abstract
Ultrasound- and microwave-assisted green synthetic strategies were applied to furnish benzofuran–oxadiazole 5ag and benzofuran–triazole 7ah derivatives in good to excellent yields (60–96%), in comparison with conventional methods (36–80% yield). These synthesized derivatives were screened for hemolysis, thrombolysis and anticancer [...] Read more.
Ultrasound- and microwave-assisted green synthetic strategies were applied to furnish benzofuran–oxadiazole 5ag and benzofuran–triazole 7ah derivatives in good to excellent yields (60–96%), in comparison with conventional methods (36–80% yield). These synthesized derivatives were screened for hemolysis, thrombolysis and anticancer therapeutic potential against an A549 lung cancer cell line using an MTT assay. Derivatives 7b (0.1%) and 5e (0.5%) showed the least toxicity against RBCs. Hybrid 7f showed excellent thrombolysis activity (61.4%) when compared against reference ABTS. The highest anticancer activity was displayed by the 5d structural hybridwith cell viability 27.49 ± 1.90 and IC50 6.3 ± 0.7 μM values, which were considerably lower than the reference drug crizotinib (IC50 8.54 ± 0.84 μM). Conformational analysis revealed the spatial arrangement of compound 5d, which demonstrated its significant potency in comparison with crizotinib; therefore, scaffold 5d would be a promising anticancer agent on the basis of cytotoxicity studies, as well as in silico modeling studies. Full article
(This article belongs to the Special Issue Heterocyclic Compounds: Design, Synthesis, and Applications)
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22 pages, 5871 KiB  
Article
Novel Pyridothienopyrimidine Derivatives: Design, Synthesis and Biological Evaluation as Antimicrobial and Anticancer Agents
by Eman M. Mohi El-Deen, Manal M. Anwar, Amina A. Abd El-Gwaad, Eman A. Karam, Mohamed K. El-Ashrey and Rafika R. Kassab
Molecules 2022, 27(3), 803; https://doi.org/10.3390/molecules27030803 - 26 Jan 2022
Cited by 10 | Viewed by 2684
Abstract
The growing risk of antimicrobial resistance besides the continuous increase in the number of cancer patients represents a great threat to global health, which requires intensified efforts to discover new bioactive compounds to use as antimicrobial and anticancer agents. Thus, a new set [...] Read more.
The growing risk of antimicrobial resistance besides the continuous increase in the number of cancer patients represents a great threat to global health, which requires intensified efforts to discover new bioactive compounds to use as antimicrobial and anticancer agents. Thus, a new set of pyridothienopyrimidine derivatives 2a,b–9a,b was synthesized via cyclization reactions of 3-amino-thieno[2,3-b]pyridine-2-carboxamides 1a,b with different reagents. All new compounds were evaluated against five bacterial and five fungal strains. Many of the target compounds showed significant antimicrobial activity. In addition, the new derivatives were further subjected to cytotoxicity evaluation against HepG-2 and MCF-7 cancer cell lines. The most potent cytotoxic candidates (3a, 4a, 5a, 6b, 8b and 9b) were examined as EGFR kinase inhibitors. Molecular docking study was also performed to explore the binding modes of these derivatives at the active site of EGFR-PK. Compounds 3a, 5a and 9b displayed broad spectrum antimicrobial activity with MIC ranges of 4–16 µg/mL and potent cytotoxic activity with IC50 ranges of 1.17–2.79 µM. In addition, they provided suppressing activity against EGFR with IC50 ranges of 7.27–17.29 nM, higher than that of erlotinib, IC50 = 27.01 nM. Full article
(This article belongs to the Special Issue Heterocyclic Compounds: Design, Synthesis, and Applications)
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