Organoselenium Derivatives in Drug Discovery

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

Deadline for manuscript submissions: closed (15 April 2023) | Viewed by 1907

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Guest Editor
Department of Organic Chemistry, University of Seville, Sevilla, Spain
Interests: medicinal chemistry; organic synthesis; enzyme inhibitors; antiproliferative agents; anti-Alzheimer's agents; polyphenols; iminosugars; coumarins; steroids; antioxidants; organoselenium compounds
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Special Issue Information

Dear Colleagues,

Organoselenium compounds have received great attention from the scientific community, particularly since the isolation of selenoproteins, which act as natural antioxidant machinery against oxidative stress, due to the presence of selenium in their active site. This led to the consideration of selenium as an essential trace element.

Since then, a plethora of selenium-containing compounds have been prepared in many different areas, with quite diverse purposes, like building blocks in synthetic organic chemistry, structural organic chemistry, catalysis, medicinal chemistry or materials science, among others.

Regarding their biological properties, organoselenium compounds emerged as very promising pharmacophores in the development of potential new drugs; in this context, the selenoheterocyclic derivative ebselen (benzo[d][1,2]-selenazol-3(2H)-one) is currently under clinical trial evaluation.

Besides the very well-known antioxidant properties, which allow them to efficiently scavenge reactive oxygen and nitrogen species (ROS, RNS), or to mimic selenoproteins, like glutathione peroxidases (GPx), a countless number of relevant pharmacological properties have been found. Numerous organoselenium compounds exhibit antiproliferative properties, which might enable the development of new cytotoxic agents or adjuvants. Additionally, anti-inflammatory, antinociceptive, antiviral, or anti-Alzheimer’s activities have also been reported.

Therefore, the aim of this Special Issue is to provide an overview of recent pharmacological research of organoselenium compounds.

Dr. Óscar López
Guest Editor

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Keywords

  • organoselenium derivatives
  • oxidative stress
  • anticancer
  • anti-Alzheimer’s agents
  • enzymatic inhibitors
  • anti-inflammatory

Published Papers (1 paper)

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Research

16 pages, 1855 KiB  
Article
Design, Synthesis, and Biological Evaluation of Novel Hydroxamic Acid-Based Organoselenium Hybrids
by Jameelah S. Alotaibi, Yasair S. Al-Faiyz and Saad Shaaban
Pharmaceuticals 2023, 16(3), 367; https://doi.org/10.3390/ph16030367 - 28 Feb 2023
Cited by 1 | Viewed by 1539
Abstract
We report the design and synthesis of novel hydroxamic acid-tethered organoselenium (OSe) hybrids. Their antimicrobial and anticancer activities were assessed against different microbes (e.g., Candida albicans (C. albicans), Escherichia coli (E. coli), and Staphylococcus aureus (S. aureus)), [...] Read more.
We report the design and synthesis of novel hydroxamic acid-tethered organoselenium (OSe) hybrids. Their antimicrobial and anticancer activities were assessed against different microbes (e.g., Candida albicans (C. albicans), Escherichia coli (E. coli), and Staphylococcus aureus (S. aureus)), as well as liver and breast carcinomas. OSe hybrid 8 showed promising anticancer activity, with IC50 = 7.57 ± 0.5 µM against HepG2 and IC50 = 9.86 ± 0.7 µM against MCF-7 cells. Additionally, OSe compounds 8 and 15 exhibited promising antimicrobial activities, particularly against C. albicans (IA% = 91.7 and 83.3) and S. aureus (IA% = 90.5 and 71.4). The minimum inhibitory concentration (MIC) assay confirmed the potential antimicrobial activity of OSe compound 8. OSe compounds 8 and 16 displayed good antioxidant activities compared to vitamin C in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and the 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assays. These results indicate that hydroxamic acid-based organoselenium hybrids have promising biological activities such as anticancer, antimicrobial, and antioxidant properties, especially compounds 8, 13, 15, and 16, which warrant further studies. Full article
(This article belongs to the Special Issue Organoselenium Derivatives in Drug Discovery)
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