Steroid Derivatives: Design and Pharmaceutical Application

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Biologics and Biosimilars".

Deadline for manuscript submissions: closed (10 April 2025) | Viewed by 4769

Special Issue Editors


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Guest Editor
Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Sciences, University of Novi Sad, Trg Dositeja Obradovića 3, 21000 Novi Sad, Serbia
Interests: organic synthesis; chemical transformations of steroid hormones and bile acids

E-Mail Website
Guest Editor
Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Sciences, University of Novi Sad, Trg Dositeja Obradovica 3, 21000 Novi Sad, Serbia
Interests: organic synthesis; chemical transformations of steroid hormones; medicinal chemistry

Special Issue Information

Dear Colleagues,

We are pleased to invite you to contribute to the new Special Issue of Pharmaceutics entitled “Steroid Derivatives: Design and Pharmaceutical Application”. Since their discovery in the early 20th century, steroids have become one of the most widely used classes of drugs in medicine. This is due to their wide range of bioactivities, from the hormonal and antitumor to the anti-inflammatory, antiparasitic, antimicrobial, etc. At present, steroids continue to trigger scientific curiosity, and they remain one of the major subjects of medicinal chemistry and pharmacology research.

This Special Issue aims to gather the latest advancements, perspectives, and trends in natural steroids and their synthetic derivatives, particularly in both experimental and theoretical studies in medicinal chemistry, structural biology, pharmacology, pharmaceutical formulation, drug delivery, and pharmacokinetics, as well as interdisciplinary research.

In this Special Issue, original research articles and reviews are welcome. Research areas may include (but not limited to) the following:

  • Design and synthesis of novel steroidal compounds;
  • Bioactivity of natural and semi-synthetic steroids;
  • Pharmacology and toxicology of steroidal derivatives;
  • Drug delivery of steroids;
  • New pharmaceutical applications of steroids;
  • New in silico methods for analysis of potential steroid applications.

We look forward to receiving your contributions to this Special Issue entitled “Steroid Derivatives: Design and Pharmaceutical Application”.

Prof. Dr. Marija Sakač
Dr. Ivana Z. Kuzminac
Guest Editors

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Keywords

  • semi-synthetic steroid compounds
  • bioactive steroids
  • drug design
  • medicinal chemistry of steroids
  • pharmacology and toxicology
  • structure elucidation

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Published Papers (2 papers)

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Research

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19 pages, 4593 KiB  
Article
A Novel 2-Methoxyestradiol Derivative: Disrupting Mitosis Inhibiting Cell Motility and Inducing Apoptosis in HeLa Cells In Vitro
by Isaac Kinyua Njangiru, Noémi Bózsity-Faragó, Vivien Erzsébet Resch, Gábor Paragi, Éva Frank, György T. Balogh, István Zupkó and Renáta Minorics
Pharmaceutics 2024, 16(5), 622; https://doi.org/10.3390/pharmaceutics16050622 - 6 May 2024
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Abstract
The clinical application of 2-methoxyestradiol (2ME) in cancer therapy has been limited by its low solubility and rapid metabolism. Derivatives of 2ME have been synthesised to enhance bioavailability and decrease hepatic metabolism. Compound 4a, an analog of 2ME, has demonstrated exceptional pharmacological [...] Read more.
The clinical application of 2-methoxyestradiol (2ME) in cancer therapy has been limited by its low solubility and rapid metabolism. Derivatives of 2ME have been synthesised to enhance bioavailability and decrease hepatic metabolism. Compound 4a, an analog of 2ME, has demonstrated exceptional pharmacological activity, in addition to promising pharmacokinetic profile. Our study, therefore, aimed at exploring the anticancer effects of 4a on the cervical cancer cell line, HeLa. Compound 4a exhibited a significant and dose-dependent antimetastatic and antiinvasive impact on HeLa cells, as determined by wound-healing and Boyden chamber assays, respectively. Hoechst/Propidium iodide (HOPI) double staining showcased a substantial induction of apoptosis via 4a, with minimal necrotic effect. Flow cytometry revealed a significant G2/M phase arrest, accompanied by a noteworthy rise in the sub-G1 cell population, indicating apoptosis, 18 h post-treatment. Moreover, a cell-independent tubulin polymerisation assay illustrated compound 4a’s ability to stabilise microtubules by promoting tubulin polymerisation. Molecular modelling experiments depicted that 4a interacts with the colchicine-binding site, nestled between the α and β tubulin dimers. Furthermore, 4a displayed an affinity for binding to and activating ER-α, as demonstrated by the luciferase reporter assay. These findings underscore the potential of 4a in inhibiting HPV18+ cervical cancer proliferation and cellular motility. Full article
(This article belongs to the Special Issue Steroid Derivatives: Design and Pharmaceutical Application)
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Review

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37 pages, 5714 KiB  
Review
Abiraterone and Galeterone, Powerful Tools Against Prostate Cancer: Present and Perspective
by Ivana Z. Kuzminac, Andrea R. Nikolić, Marina P. Savić and Jovana J. Ajduković
Pharmaceutics 2024, 16(11), 1401; https://doi.org/10.3390/pharmaceutics16111401 - 30 Oct 2024
Cited by 1 | Viewed by 1676
Abstract
Due to the high prostate cancer incidence worldwide, the development of different methods of treatment continues to be a hot research topic. Since its first clinical application at the beginning of the 2010s, abiraterone in the form of prodrug abiraterone acetate continues to [...] Read more.
Due to the high prostate cancer incidence worldwide, the development of different methods of treatment continues to be a hot research topic. Since its first clinical application at the beginning of the 2010s, abiraterone in the form of prodrug abiraterone acetate continues to be the most used hormone derivative in the treatment of castration-resistant prostate cancer. This is the reason behind the publication of many scientific results regarding its synthesis, biological activity, metabolism, novel designed steroid derivatives based on its structure, etc. A similar steroid compound with a heterocycle in the C17 position, called galeterone, also designed to treat prostate cancer, continues to be in clinical studies, which provides further proof of the importance of these steroid derivatives. Besides prostate cancer treatment, abiraterone showed indications for possible clinical application in the treatment of breast, ovarian, lung, kidney, salivary gland, and adrenocortical cancer, congenital adrenal hyperplasia, Cushing’s syndrome, and COVID-19, while galeterone is investigated for its use against prostate, pancreatic, and breast cancer. Herein, we report a review comprising methods of synthesis, possible clinical applications, and mechanisms of action, as well as structures and bioactivities of derivatives of these two important steroids. Full article
(This article belongs to the Special Issue Steroid Derivatives: Design and Pharmaceutical Application)
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