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Pharmaceuticals
Special Issues
Chemotherapeutic and Targeted Drugs in Antitumor Therapy
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Chemotherapeutic and Targeted Drugs in Antitumor Therapy

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

Deadline for manuscript submissions: 15 February 2026 | Viewed by 810

Special Issue Editors

Dr. Angéla Takács

E-Mail Website
Guest Editor
Department of Genetics, Cell and Immunobiology, Semmelweis University, Nagyvárad tér 4, H-1089 Budapest, Hungary
Interests: drug discovery; combination studies; multiple myeloma; real-time imaging; impedance-based cell viability assay
Dr. László Kőhidai

E-Mail Website
Guest Editor
Department of Genetics, Cell and Immunobiology, Semmelweis University, Nagyvárad tér 4, H-1089 Budapest, Hungary
Interests: cell physiology; drug targeting; chemotaxis; apoptosis; impedimetry assays
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Classical chemotherapies non-selectively target rapidly dividing cells, affecting both cancerous and healthy tissues. In contrast, targeted therapies are designed to act on specific cell populations characterized by well-defined molecular markers (e.g., trastuzumab targeting HER2-positive cells). The benefits of targeted therapies have revolutionized oncology by enabling more personalized and effective treatments. Nevertheless, the role of classical chemotherapeutic agents remains essential and continues to form the backbone of many cancer treatment regimens.  According to the World Health Organization, cancer is a leading cause of death worldwide (around 10 million deaths per year); therefore, intensive research of either new chemotherapeutics, targeted therapies or their combination is crucial.

We invite researchers to contribute to this Special Issue "Chemotherapeutic and Targeted Drugs in Antitumor Therapy," which aims to provide a comprehensive overview of novel antitumor treatments and the latest findings to outline the possible future perspectives. Submissions focusing on innovative therapeutic strategies—both in vitro and in vivo—are highly encouraged.

Dr. Angéla Takács
Dr. László Kőhidai
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. Pharmaceuticals 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

  • cancer
  • drug discovery
  • small-molecule drugs
  • targeted therapy
  • combination therapy
  • synergism
  • selectivity
  • immunotherapy
  • precision medicine

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Published Papers (1 paper)

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Research

27 pages, 5600 KB  
Article
Comparative Study of Ferrocene- and Indene-Based Tamoxifen Derivatives of Different Molecular Flexibility on High-Mortality Cancer Cell Lines
by Márton Kalabay, Zsófia Szász, Eszter Lajkó, Bálint Bagu, Éva Pállinger, Cintia Duró, Tamás Jernei, Antal Csámpai, Angéla Takács and László Kőhidai
Pharmaceuticals 2025, 18(9), 1417; https://doi.org/10.3390/ph18091417 - 20 Sep 2025
Viewed by 95
Abstract
Tamoxifen is a well-established selective estrogen receptor modulator (SERM) widely used in breast cancer treatment, yet its efficacy varies across tumor types. To enhance its antitumor potential, we previously synthesized and investigated novel ferrocene-linked (T5, T15) derivatives. This publication is a close continuation [...] Read more.
Tamoxifen is a well-established selective estrogen receptor modulator (SERM) widely used in breast cancer treatment, yet its efficacy varies across tumor types. To enhance its antitumor potential, we previously synthesized and investigated novel ferrocene-linked (T5, T15) derivatives. This publication is a close continuation of this work, introducing a new indene-based (T6) derivative. Objectives: The main aim of this study was to further broaden our knowledge of the mechanism behind the increased antitumor effect of the ferrocene-linked drugs (T5 and T15) and compare it with a new, indene-based tamoxifen derivative, T6. The indene moiety was selected as a rigid, hydrophobic aromatic unit to probe pharmacological effects independent of ferrocene’s redox activity. Methods: The compounds were tested on MCF7, MDA-MB231 and PANC1 cells. Cell viability was assessed with the AlamarBlue assay and the xCELLigence SP system. Reactive oxygen species (ROS) production was measured with the ROS Glo assay. Flow cytometry and RT-qPCR experiments were conducted to assess apoptosis and ROS regulation as well. Results: The modified compounds demonstrated an increased cell-viability-decreasing effect in breast (MCF7, MDA-MB-231) and pancreatic (PANC1) cancer cell lines, influencing both estrogen-receptor-dependent and -independent pathways. T6 led to G2/M phase arrest in PANC1 cells. Beyond cell cycle disruption, these derivatives significantly elevated ROS levels, contributing to apoptosis. Conclusions: Our findings suggest that these structural modifications retain tamoxifen’s pharmacophore properties while expanding its mechanism of action, particularly through universal interactions independent of the ER status of tumor cells. The enhanced antitumor effects highlight the potential of these derivatives as promising candidates for improved cancer therapies. Full article
(This article belongs to the Special Issue Chemotherapeutic and Targeted Drugs in Antitumor Therapy)
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