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Biomedicines
Special Issues
Anti-Cancer Agents: Synthesis and Evaluation of Pharmacological Activity
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Anti-Cancer Agents: Synthesis and Evaluation of Pharmacological Activity

A special issue of Biomedicines (ISSN 2227-9059). This special issue belongs to the section "Drug Discovery, Development and Delivery".

Deadline for manuscript submissions: 28 February 2027 | Viewed by 1907

Editor

Dr. Sureshbabu Popuri

E-Mail Website
Guest Editor
Department of Medicinal Chemistry, University of Kansas, Lawrence, KS 66045, USA
Interests: organic synthesis; bio-inorganic chemistry; metal complexes; anticancer agents; biomolecule interactions

Special Issue Information

Dear Colleagues,

The search for effective and selective anticancer agents remains a primary challenge in drug discovery and development. Chemotherapy, a mainstay in cancer treatment, often suffers from drawbacks such as poor selectivity, drug resistance, and severe side effects. As such, there is a growing need to develop novel compounds that can efficiently target cancer cells while sparing normal tissues.

This Special Issue focuses on the synthesis, characterization, and pharmacological evaluation of new anticancer agents, emphasizing small molecules, natural products, metal complexes, and hybrid compounds. The contributions aim to showcase the latest progress in designing compounds with enhanced antiproliferative activity, reduced toxicity, and improved selectivity against various cancer types.

The studies reflect a multidisciplinary approach, encompassing organic and medicinal chemistry, computational drug design, structure–activity relationship (SAR) investigations, and in vitro and in vivo testing. This collection highlights strategies to target key signaling cascades, inhibit enzyme activity, induce apoptosis, or interfere with the cell cycle in tumor cells. Furthermore, it underscores the potential of structure modifications to maximize potency while minimizing side effects.

Together, these investigations underscore the significance of rational drug design and extensive biological evaluation in developing effective anticancer agents. This Special Issue aims to provide important insights and foster future innovations in the field of anticancer drug discovery.

Dr. Sureshbabu Popuri
Guest Editor

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 250 words) can be sent to the Editorial Office for assessment.

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-anonymized peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Biomedicines 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 2600 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

  • anticancer agents
  • synthesis
  • pharmacological evaluation
  • medicinal chemistry
  • small molecules
  • metal complexes
  • structure–activity relationship (SAR)
  • cytotoxic activity
  • apoptosis
  • drug discovery
  • chemotherapy

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Further information on MDPI's Special Issue policies can be found here.

Published Papers (2 papers)

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Research

12 pages, 1872 KB  
Article
A Boronic Acid-Based Glutamine Analog Forms a Covalent Adduct with Kidney-Type Glutaminase and Suppresses Triple-Negative Breast Cancer Cell Proliferation
by Thiruselvam Viswanathan, Dinesh Devadoss, Achyuta Nagaraj, Barry P. Rosen, Hitendra S. Chand and Venkadesh Sarkarai Nadar
Biomedicines 2026, 14(5), 1100; https://doi.org/10.3390/biomedicines14051100 - 13 May 2026
Viewed by 531
Abstract
Background: Cancer cells exhibit metabolic reprogramming characterized by increased dependence on glutamine to sustain rapid proliferation and biosynthetic demands. Kidney-type glutaminase (KGA), which catalyzes the first and rate-limiting step of glutamine metabolism, represents a promising therapeutic target, particularly in triple-negative breast cancer [...] Read more.
Background: Cancer cells exhibit metabolic reprogramming characterized by increased dependence on glutamine to sustain rapid proliferation and biosynthetic demands. Kidney-type glutaminase (KGA), which catalyzes the first and rate-limiting step of glutamine metabolism, represents a promising therapeutic target, particularly in triple-negative breast cancer (TNBC), an aggressive sub-type lacking effective targeted therapies. This study evaluated 2-amino-4-boronobutyric acid (ABBA), a boronic acid-containing glutamine analog, as a potential KGA inhibitor with anticancer activity. Methods: KGA inhibition was assessed using a fluorometric enzymatic assay. Cytotoxic effects were examined in multiple TNBC cell lines. Covalent docking and molecular simulation analysis were performed to characterize interactions between ABBA and the KGA active site. Results: ABBA potently inhibited KGA activity, with an IC50 of approximately 1.0 μM, demonstrating greater efficacy than several non-proteinogenic amino acid analogs. ABBA induced dose-dependent cytotoxicity across multiple TNBC cell lines, with pronounced sensitivity observed in basal sub-type cells and cellular sensitivity correlated with KGA expression levels. Expression of γ-glutamyl transpeptidase 1 (GGT1) was negligible, and, excluding any off-target effects, the observed anticancer effects are primarily attributed to KGA inhibition. Docking analysis indicated that ABBA forms a reversible covalent adduct with the catalytic Ser286 residue of KGA in a boronate tetrahedral geometry resembling transition-state mimics, while molecular simulation demonstrated stabilization of the complex through hydrogen bonding and electrostatic interactions. Conclusions: ABBA is a potent boron-based glutaminase inhibitor with therapeutic potential for targeting glutamine metabolism in TNBC. Further structural optimization and in vivo evaluation are warranted to advance ABBA toward therapeutic development. Full article
(This article belongs to the Special Issue Anti-Cancer Agents: Synthesis and Evaluation of Pharmacological Activity)
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30 pages, 4906 KB  
Article
Secosteroid–2-Pyrazoline Hybrids: Design, Synthesis, Biological Evaluation and Development of Therapeutic Combinations Against ERα-Positive Breast Cancer Cells
by Alexey I. Ilovaisky, Alexander M. Scherbakov, Fedor B. Bogdanov, Dumitru Miciurov, Elena I. Chernoburova, Valentina M. Merkulova, Eugene I. Bozhenko, Andrey S. Dmitrenok, Diana I. Salnikova, Danila V. Sorokin, Alvina I. Khamidullina, Mikhail A. Krasil’nikov, Igor V. Zavarzin and Alexander O. Terent’ev
Biomedicines 2025, 13(12), 3057; https://doi.org/10.3390/biomedicines13123057 - 11 Dec 2025
Cited by 1 | Viewed by 873
Abstract
Background/Objectives: Breast cancer remains one of the most prevalent and life-threatening malignancies worldwide. This study describes the design and biological evaluation of a series of secosteroid–2-pyrazoline hybrids as novel antitumor agents against ERα-positive breast cancer cell lines MCF-7 and T47D. Methods: A [...] Read more.
Background/Objectives: Breast cancer remains one of the most prevalent and life-threatening malignancies worldwide. This study describes the design and biological evaluation of a series of secosteroid–2-pyrazoline hybrids as novel antitumor agents against ERα-positive breast cancer cell lines MCF-7 and T47D. Methods: A simple and efficient method for synthesizing secosteroid–2-pyrazoline hybrids was developed starting from 13α-hydroxy-3-methoxy-13,17-secoestra-1,3,5(10)-triene-17-oic acid hydrazide and 1,3-diketones. The resulting secosteroid derivatives were evaluated against hormone-dependent MCF-7 and T47D breast cancer cells. Furthermore, the selectivity and effects of three lead compounds on signaling pathways in MCF-7 cells were examined. Flow cytometry was used to assess the cell-cycle distribution of MCF-7 cells treated with the lead compound. Results: Among the synthesized hybrids, compounds 3f, 3j, and 3k exhibited potent antiproliferative activity with IC50 values of 0.2–0.5 μM against breast cancer cells, while demonstrating very low cytotoxicity towards normal cells (IC50 > 25 μM), indicating a favorable safety profile. The antitumor activity of lead compound 3j was additionally investigated in combination with standard chemotherapeutics, docetaxel and doxorubicin, yielding synergistic effects. The lead compounds showed a dual mechanism of action by inhibiting S6 kinase and promoting Bcl-2 phosphorylation at 0.9 μM, without significantly affecting hormonal breast cancer targets such as ERα, GREB1, and AR. Compound 3j induced apoptosis accompanied by a reduction of the G1/G0 phase in MCF-7 cells. Conclusions: These findings highlight secosteroid–2-pyrazoline hybrids as promising candidates for the development of next-generation breast cancer therapeutics targeting apoptosis and S6K signaling pathways. Full article
(This article belongs to the Special Issue Anti-Cancer Agents: Synthesis and Evaluation of Pharmacological Activity)
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