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Dr. Davide Moi
Department of Life and Environmental Sciences, University of Cagliari, University Campus, S.P. 8 CA, 09042 Monserrato, Italy
Prof. Dr. Daniele Passarella
Department of Chemistry, University of Milan, Via Golgi 19, 20133 Milano, Italy
Department of Chemistry, University of Milan, Via Golgi 19, 20133 Milan, Italy
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Design, Synthesis and Biological Evaluation of Novel Small Molecules as Multi-target Enzyme Inhibitors

Abstract submission deadline
30 September 2024
Manuscript submission deadline
31 January 2025
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1048

Topic Information

Dear Colleagues,

We are delighted to announce the initiation of a Topic, "Design, Synthesis and Biological Evaluation of Novel Small Molecules as Multi-target Enzyme Inhibitors", dedicated to exploring the dynamic intersection of synthetic organic chemistry and biology, with profound implications for diverse medical applications.

Within this specialized topic, our focus is on the synthesis and biological assessment of novel small molecules designed to inhibit multiple enzymes concurrently. Multi-target enzyme inhibitors offer a comprehensive treatment approach by simultaneously targeting multiple disease-related pathways, enhancing therapeutic efficacy. Their ability to mitigate drug resistance, improve selectivity, and potentially provide synergistic effects makes them promising candidates for treating complex diseases. Additionally, the versatility of these inhibitors allows for a more personalized treatment strategy, addressing the multifactorial origins of various medical conditions.

The synthesis process involves optimizing for favorable pharmacokinetic properties and target specificity, leading to a varied library of compounds. The potential applications of the target inhibitors extend into critical areas of medical research, including neurological disorders, the antimicrobial field, antidiabetic therapies, and so on.

We also welcome investigations into novel synthetic methodologies, recognizing their importance in developing innovative strategies to access multi-target inhibitors. Contributions in the form of reviews and original research papers are encouraged for publication. We invite your participation in creating a comprehensive collection of articles, promoting a deeper understanding of the synthesis and evaluation of small molecules with multi-target enzyme-inhibitory properties and the development of novel synthetic routes.

We eagerly anticipate and welcome your valuable contributions to advancing the discourse surrounding this exciting and rapidly evolving field.

Dr. Davide Moi
Prof. Dr. Daniele Passarella
Dr. Andrea Citarella
Topic Editors

Keywords

  • organic synthesis
  • medicinal chemistry
  • enzyme inhibitors
  • synthetic methodologies
  • bioactive compounds
  • drug design
  • molecular modelling
  • drug discovery

Participating Journals

Journal Name Impact Factor CiteScore Launched Year First Decision (median) APC
BioChem
biochem 		- - 2021 54 Days CHF 1000 Submit
Biomolecules
biomolecules 		5.5 8.3 2011 16.9 Days CHF 2700 Submit
Current Issues in Molecular Biology
cimb 		3.1 2.4 1999 13.5 Days CHF 2200 Submit
Molecules
molecules 		4.6 6.7 1996 14.6 Days CHF 2700 Submit
Pharmaceutics
pharmaceutics 		5.4 6.9 2009 14.2 Days CHF 2900 Submit
Scientia Pharmaceutica
scipharm 		2.5 6.4 1930 22.7 Days CHF 1000 Submit

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Published Papers (1 paper)

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18 pages, 2383 KiB  
Article
The Effects of the Steroids 5-Androstenediol and Dehydroepiandrosterone and Their Synthetic Derivatives on the Viability of K562, HeLa, and Wi-38 Cells and the Luminol-Stimulated Chemiluminescence of Peripheral Blood Mononuclear Cells from Healthy Volunteers
by Mikhail N. Sokolov, Vladimir V. Rozhkov, Maria E. Uspenskaya, Darya N. Ulchenko, Vladimir I. Shmygarev, Vladimir M. Trukhan, Andrei V. Churakov, Nikolay L. Shimanovsky and Tatiana A. Fedotcheva
Biomolecules 2024, 14(3), 373; https://doi.org/10.3390/biom14030373 - 19 Mar 2024
Viewed by 675
Abstract
In order to evaluate the role of substituents at 3-C and 17-C in the cytotoxic and cytoprotective actions of DHEA and 5-AED molecules, their derivatives were synthesized by esterification using the corresponding acid anhydrides or acid chlorides. As a result, seven compounds were [...] Read more.
In order to evaluate the role of substituents at 3-C and 17-C in the cytotoxic and cytoprotective actions of DHEA and 5-AED molecules, their derivatives were synthesized by esterification using the corresponding acid anhydrides or acid chlorides. As a result, seven compounds were obtained: four DHEA derivatives (DHEA 3-propionate, DHEA 3-butanoate, DHEA 3-acetate, DHEA 3-methylsulfonate) and three 5-AED derivatives (5-AED 3-butanoate, 5-AED 3,17-dipropionate, 5-AED 3,17-dibutanoate). All of these compounds showed micromolar cytotoxic activity toward HeLa and K562 human cancer cells. The maximum cytostatic effect during long-term incubation for five days with HeLa and K562 cells was demonstrated by the propionic esters of the steroids: DHEA 3-propionate and 5-AED 3,17-dipropionate. These compounds stimulated the growth of normal Wi-38 cells by 30–50%, which indicates their cytoprotective properties toward noncancerous cells. The synthesized steroid derivatives exhibited antioxidant activity by reducing the production of reactive oxygen species (ROS) by peripheral blood mononuclear cells from healthy volunteers, as demonstrated in a luminol-stimulated chemiluminescence assay. The highest antioxidant effects were shown for the propionate ester of the steroid DHEA. DHEA 3-propionate inhibited luminol-stimulated chemiluminescence by 73% compared to the control, DHEA, which inhibited it only by 15%. These data show the promise of propionic substituents at 3-C and 17-C in steroid molecules for the creation of immunostimulatory and cytoprotective substances with antioxidant properties. Full article
(This article belongs to the Topic Design, Synthesis and Biological Evaluation of Novel Small Molecules as Multi-target Enzyme Inhibitors)
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