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Advances in Small-Molecule Cancer Therapeutics: Current Challenges and Future Perspectives

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 30 April 2027 | Viewed by 346

Editors


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Guest Editor
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskişehir 26470, Turkey
Interests: anticancer drug discovery; cancer-related kinases; drugs acting on cell death networks; small molecules; rational drug design; medicinal chemistry; heterocyclic chemistry; computational chemistry
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Guest Editor
Department of Biochemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey
Interests: cancer; cancer-related targets; cell signaling pathways; cell death networks; biochemistry

Special Issue Information

Dear Colleagues,

Cancer is a group of diseases characterized by the rapid and uncontrolled proliferation of abnormal cells. Despite significant advances in diagnosis, prevention, and treatment, it remains a major global public health challenge, causing millions of deaths worldwide.

In the pursuit of more effective therapies that overcome the limitations of conventional chemotherapy, targeted therapies have emerged as a promising approach to maximize therapeutic efficacy while minimizing adverse effects. Continuous advances in understanding the multifactorial pathogenesis of cancer have enabled the identification of novel molecular targets and the subsequent development of targeted therapeutics. In this context, small molecules offer several advantages over macromolecules, including favorable pharmacokinetic properties, cost-effectiveness, and improved patient compliance.

This Special Issue will focus on current challenges, emerging trends, and future directions in small-molecule anticancer drug discovery. We cordially invite you to submit research articles and reviews related to the discovery of small molecules for cancer therapy.

We look forward to receiving your contributions.

Prof. Dr. Mehlika Dilek Altıntop
Prof. Dr. Gülşen Akalın Çiftçi
Guest Editors

Manuscript Submission Information

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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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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
  • targeted therapy
  • anticancer drug discovery
  • lead identification
  • small molecules
  • cancer-related targets
  • signaling pathways in cancer
  • emerging approaches to anticancer drug design
  • targeted drug delivery

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Published Papers (1 paper)

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Research

19 pages, 1833 KB  
Article
Cisplatin and ε-Viniferin Synergistically Modulate Oxidative Stress in HeLa Cells: Implications for Redox Modulation in Cervical Cancer Cells
by Tayyar Görkem Sayer, Gamze Yılmaz and Filiz Özdemir
Molecules 2026, 31(14), 2409; https://doi.org/10.3390/molecules31142409 - 8 Jul 2026
Viewed by 106
Abstract
This study investigates the combined effects of cisplatin (CDDP) and ε-viniferin (ε-VNF), a natural stilbenoid, on oxidative stress and apoptosis in HeLa cells. Cytotoxicity was assessed using the MTT assay, and IC50 values were determined as 28 µM for CDDP and 21 [...] Read more.
This study investigates the combined effects of cisplatin (CDDP) and ε-viniferin (ε-VNF), a natural stilbenoid, on oxidative stress and apoptosis in HeLa cells. Cytotoxicity was assessed using the MTT assay, and IC50 values were determined as 28 µM for CDDP and 21 µM for ε-VNF. Synergistic and antagonistic combination ratios of these doses were tested. Oxidative stress was evaluated via Total Oxidant Status (TOS), Total Antioxidant Status (TAS), Oxidative Stress Index (OSI), Superoxide Dismutase (SOD), Reduced Glutathione (GSH), and Malondialdehyde (MDA). Apoptosis was measured using Annexin V-FITC/PI staining and caspase-9 activation assays. TAS levels significantly increased in all combination groups compared to the control (control: 266.7 ± 0.1 µmol/L; 20% combo: 2466.7 ± 1.0 µmol/L). OSI values decreased accordingly (control: 22.5 ± 7.1; 10% combo: 1.6 ± 0.5). GSH levels decreased in the combination groups (e.g., 20%: 0.8 ± 0.2 µM vs. control: 1.4 ± 0.1 µM), while MDA levels increased (20%: 3.8 ± 0.5 µM vs. control: 0.5 ± 0.1 µM). Caspase-9 positive cells increased markedly (20%: 55.0% vs. control: 13.2%), supporting activation of the mitochondrial apoptotic pathway. Annexin V analysis revealed increased late apoptosis (20%: 76.1%) and early apoptosis (20%: 17.0%). Full article
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