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New Anti-cancer Agents: Design, Synthesis and Applications
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New Anti-cancer Agents: Design, Synthesis and Applications

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: 20 September 2025 | Viewed by 1380

Special Issue Editor

Dr. Robert Czarnomysy

E-Mail Website
Guest Editor
Department of Synthesis and Technology of Drugs, Medical University of Bialystok, Kilinskiego 1, 15-089 Bialystok, Poland
Interests: anti-cancer agents; medicinal chemistry; drug design and synthesis; drug delivery systems

Special Issue Information

Dear Colleagues,

To date, 317 anticancer drugs have been licensed, with 286 approved by the FDA, and 212 approved by the EMA. These drugs can be classified according to their mechanism of action, indication, or chemical structure. Most chemotherapeutic agents cause side effects, which limit their use. Consequently, there is a growing need for research focused on designing novel targeted drugs. This Special Issue of IJMS is devoted to all stages of the process of developing new drugs, including design, synthesis, and pharmacological evaluation of anti-cancer activity in novel therapeutics. Submissions of both research and review articles are welcome for this Special Issue.

This Special Issue is supervised by Dr. Robert Czarnomysy and assisted by our Topical Advisory Panel Member Dr. Anna Szymanowska (szymanowska_anna@wp.pl; Department of Biotechnology, Medical University of Bialystok, Kilinskiego 1, 15-089 Bialystok, Poland).

Dr. Robert Czarnomysy
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 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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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

  • anti-cancer drugs
  • cancer drug development
  • cancer therapy
  • rational drug design
  • structure–activity relationship
  • cancer therapeutics
  • cytotoxicity
  • apoptosis
  • anti-tumor activity

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Published Papers (2 papers)

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Research

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22 pages, 4738 KiB  
Article
Tri-Phenyl-Phosphonium-Based Nano Vesicles: A New In Vitro Nanomolar-Active Weapon to Eradicate PLX-Resistant Melanoma Cells
by Silvana Alfei, Carola Torazza, Francesca Bacchetti, Maria Grazia Signorello, Mario Passalacqua, Cinzia Domenicotti and Barbara Marengo
Int. J. Mol. Sci. 2025, 26(7), 3227; https://doi.org/10.3390/ijms26073227 - 30 Mar 2025
Viewed by 388
Abstract
Cutaneous metastatic melanoma (CMM) is the most aggressive form of skin cancer, with characteristics including a poor prognosis, chemotherapy-induced secondary tumorigenesis, and the emergence of drug resistance. Our recent study demonstrated that triphenyl phosphonium (TPP)-based nanovesicles (BPPB), which have amphiphilic properties, exert potent [...] Read more.
Cutaneous metastatic melanoma (CMM) is the most aggressive form of skin cancer, with characteristics including a poor prognosis, chemotherapy-induced secondary tumorigenesis, and the emergence of drug resistance. Our recent study demonstrated that triphenyl phosphonium (TPP)-based nanovesicles (BPPB), which have amphiphilic properties, exert potent ROS-dependent anticancer effect against PLX4032 (PLX)-sensitive MeOV BRAFV600E and MeTRAV BRAFV600D mutant cell lines, evidencing more marked efficacy on MeOV cells. Here, taking advantage of this in vitro model, the antitumoral effect of BPPB was tested on PLX-resistant (PLX-R) MeOV BRAFV600E and MeTRAV BRAFV600D mutant cell lines to find a new potential strategy to fight melanoma therapy resistance. Specifically, we investigated both its effects on cell viability in dose- and time-dependent experiments and those on ROS generation. Our results show that BPPB exerted strong antiproliferative effects, regardless of their acquired resistance of cells to PLX, that correlated with ROS overproduction for 24 h treatments only. Moreover, in terms of cell viability, PLX-R MeTRAV cells demonstrated a remarkably higher tolerance to 24 h BPPB treatment than PLX-R MeOV. On the contrary, BPPB exposure for longer periods induced similar responses in both cell lines (IC50 = 87.8–106.5 nM on MeOV and 81.0–140.6 nM on MeTRAV). Notably, BPPB cytotoxicity on non-tumorigenic human keratinocytes (HaCaT) was low, thus establishing that BPPB is appreciably selective for CMM cells, allowing for selectivity index values (SIs) up to 11.58. Furthermore, the BPPB concentration causing 50% hemolysis (HC50) was found to be 16–173 and 4–192-fold higher than the IC50 calculated for PLX-R MeOV and MeTRAV cells, respectively. Correlation studies established that BPPB exerts cytotoxic effects on PLX-R MeOV and MeTRAV cells by a time-dependent mechanism, while a concentration-dependent mechanism was observed only at 24 h of exposure. Finally, a ROS-dependent mechanism can be assumed only in PLX-R MeTRAV cells in 72 h treatment. Full article
(This article belongs to the Special Issue New Anti-cancer Agents: Design, Synthesis and Applications)
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Review

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20 pages, 874 KiB  
Review
The Revolution of Targeted Therapies in Thyroid Cancer Treatment: Present and Future Promising Anti-Cancer Drugs
by Sara Gil-Bernabé, Lucía García-DeLaFuente and Ginesa García-Rostán
Int. J. Mol. Sci. 2025, 26(8), 3663; https://doi.org/10.3390/ijms26083663 - 12 Apr 2025
Viewed by 569
Abstract
Thyroid cancer prevalence has increased in the last few decades. Whereas the majority of well-differentiated histotypes have effective therapeutic options, the most advanced cases lacked successful treatment until recent years. Genomic alterations have emerged as targets for new anti-cancer drugs. This molecular knowledge [...] Read more.
Thyroid cancer prevalence has increased in the last few decades. Whereas the majority of well-differentiated histotypes have effective therapeutic options, the most advanced cases lacked successful treatment until recent years. Genomic alterations have emerged as targets for new anti-cancer drugs. This molecular knowledge is gradually being translated into sophisticated approaches for the stratification, management, and therapies of patients with thyroid carcinomas. The genomic characterisation of tumours in clinical assistance serves as a tool for enhancing the prognostic assessment of patients with thyroid cancer and predicting their responses to the agents. The MAPK pathway is the most predominantly activated molecular route in this cancer. Several drugs have been developed to inhibit this pathway at different levels. However, the acquired resistance that emerges is the main problem in their use. Other strategies targeting not only driver mutations but also those that confer aggressive behaviour on tumours can be potential targetable options. Due to the new therapies, patients with the most aggressive histotypes have improved survival rates. Adverse events, although manageable, have a high prevalence among the current therapies. Selective inhibitors, immunotherapies, and the combination of both will play a pivotal role in the treatment and the improvements in overall survival in thyroid cancer patients. Full article
(This article belongs to the Special Issue New Anti-cancer Agents: Design, Synthesis and Applications)
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