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Emerging Heterocycles

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Biochemistry".

Deadline for manuscript submissions: closed (31 March 2024) | Viewed by 549

Special Issue Editors


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Guest Editor
School of Chemistry, University of New South Wales (UNSW Sydney), Sydney, NSW 2052, Australia
Interests: heterocyclic chemistry; synthetic organic chemistry; natural products chemistry; new indole-based scaffolds; synthetic methodologies
Special Issues, Collections and Topics in MDPI journals

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Guest Editor

Special Issue Information

Dear Colleagues,

Heterocycles are abundant in nature and play important roles in all aspects of life. The synthesis of natural and unnatural heterocyclic molecules is becoming increasingly significant as new scaffolds are required to overcome the increasing problems of drug resistance. Heterocycles are also key building blocks for the construction of the next generation of materials.

The scope of this Special Issue is intentionally broad and inclusive and encompasses any type of paper (review, original paper, communication, perspective paper) regarding structural and/or functional studies, reactions, and applications of heterocycles and their biological activity and biosynthesis. In addition, new methodological approaches are the topics to focus on.

Prof. Dr. David StC Black
Prof. Dr. Naresh Kumar
Guest Editors

Manuscript Submission Information

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Keywords

  • synthesis
  • reactions
  • applications
  • biological activity
  • medicinal chemistry
  • natural products
  • alkaloids
  • new methodology

Published Papers (1 paper)

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Research

26 pages, 4355 KiB  
Article
Novel Tetracyclic Azaphenothiazines with the Quinoline Ring as New Anticancer and Antibacterial Derivatives of Chlorpromazine
by Małgorzata Jeleń, Dagmara Otto-Ślusarczyk, Beata Morak-Młodawska and Marta Struga
Int. J. Mol. Sci. 2024, 25(8), 4148; https://doi.org/10.3390/ijms25084148 - 09 Apr 2024
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Abstract
Phenothiazine derivatives are widely studied in various fields such as biology, chemistry, and medicine research because of their pharmaceutical effects. The first compound used successfully in the treatment of psychosis was a phenthiazine derivative, chlorpromazine. Apart from its activity in neurons, chlorpromazine has [...] Read more.
Phenothiazine derivatives are widely studied in various fields such as biology, chemistry, and medicine research because of their pharmaceutical effects. The first compound used successfully in the treatment of psychosis was a phenthiazine derivative, chlorpromazine. Apart from its activity in neurons, chlorpromazine has also been reported to display anticancer and antibacterial properties. In this study, we present the synthesis and research on the activity of A549, MDA, MiaPaCa, PC3, and HCT116 cancer cell lines and of S. aureus, S. epidermidis, E. coli, and P. aeruginosa bacterial strains against a series of new tetracyclic chlorpromazine analogues containing a quinoline scaffold in their structure instead of the benzene ring and various substituents at the thiazine nitrogen. The structure of these novel molecules has been determined by 1H NMR, 13C NMR, and HRMS spectral techniques. The seven most active of the twenty-four new chlorpromazine analogues tested were selected to study the mechanism of cytotoxic action. Their ability to induce apoptosis or necrosis in cancer cells was assessed by flow cytometry analysis. The results obtained confirmed the proapoptotic activity of selected compounds, especially in terms of inducing late apoptosis or necrosis in cancer cell lines A549, MiaPaCa-2, and HCT-116. Furthermore, studies on the induction of cell cycle arrest suggest that the new chlorpromazine analogues exert antiproliferative effects by inducing cell cycle arrest in the S phase and, consequently, apoptosis. Full article
(This article belongs to the Special Issue Emerging Heterocycles)
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