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: 1 October 2024 | Viewed by 766

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

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

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

Published Papers (1 paper)

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Research

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
Viewed by 566
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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