Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
6.1
4.3
Journals
Pharmaceuticals
Special Issues
Advances in Hybrid Anticancer Drugs: Innovations and Therapeutic Potential
share announcement

Advances in Hybrid Anticancer Drugs: Innovations and Therapeutic Potential

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

Deadline for manuscript submissions: 25 September 2025 | Viewed by 310

Special Issue Editor

Dr. Dmytro Khylyuk

E-Mail Website
Guest Editor
Chair and Department of Organic Chemistry, Medical University of Lublin, 4A Chodzki Street, 20-093 Lublin, Poland
Interests: anticancer drugs; molecular docking and dynamics; 4-thiazolidinones

Special Issue Information

Dear Colleagues, 

Despite significant advances in anticancer agents, cancer remains a major medical challenge due to the complexity and heterogeneity of tumor cells, as well as their capacity to develop treatment resistance. Researchers are therefore exploring novel approaches to create more effective and safer drugs, with a particularly promising strategy focused on hybrid molecules that combine multiple mechanisms of action or enhance existing therapies.

Developing hybrid anticancer agents entails combining multiple pharmacophores and privileged scaffolds into a single molecule to overcome drug resistance, enhance cytotoxicity against cancer cells, and improve selectivity. Such strategies aim to achieve a comprehensive anticancer effect by simultaneously targeting two or more key pathogenic pathways.

This Special Issue aims to showcase the latest developments in hybrid anticancer drugs, including innovative synthetic methods, therapeutic potential, and mechanistic insights. We especially welcome submissions featuring targeted drug design aimed at influencing specific pathogenetic pathways, as well as research presenting both in vitro and in vivo findings and robust in silico evidence supporting cytotoxic activity and predicted mechanisms of action.

We invite original research and review articles that detail novel approaches, discuss emerging trends, and propose pathways for future discovery and development of new, more effective anticancer drugs.

Dr. Dmytro Khylyuk
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. 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

  • drug design
  • molecular hybrids
  • anticancer agents
  • privileged scaffold
  • multiple mechanisms of action

Benefits of Publishing in a Special Issue

  • Ease of navigation: Grouping papers by topic helps scholars navigate broad scope journals more efficiently.
  • Greater discoverability: Special Issues support the reach and impact of scientific research. Articles in Special Issues are more discoverable and cited more frequently.
  • Expansion of research network: Special Issues facilitate connections among authors, fostering scientific collaborations.
  • External promotion: Articles in Special Issues are often promoted through the journal's social media, increasing their visibility.
  • Reprint: MDPI Books provides the opportunity to republish successful Special Issues in book format, both online and in print.

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

Published Papers (1 paper)

Order results
Result details
Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:

Research

15 pages, 1915 KiB  
Communication
Performance of Imidazoquinoline Glycoconjugate BAIT628 as a TLR7 Agonist Prodrug for Prostate Cancer
by Seyedeh A. Najibi, S. M. Al Muied Pranto, Muhammad Haroon, Amy E. Nielsen and Rock J. Mancini
Pharmaceuticals 2025, 18(6), 804; https://doi.org/10.3390/ph18060804 - 27 May 2025
Viewed by 180
Abstract
Despite broad anti-cancer efficacy as Toll-Like Receptor (TLR) 7/8 agonists, imidazoquinolines remain limited in use via systemic administration or in situ vaccination therapies due to inflammatory toxicity. One approach to address this challenge involves better targeting the action of imidazoquinolines by caging them [...] Read more.
Despite broad anti-cancer efficacy as Toll-Like Receptor (TLR) 7/8 agonists, imidazoquinolines remain limited in use via systemic administration or in situ vaccination therapies due to inflammatory toxicity. One approach to address this challenge involves better targeting the action of imidazoquinolines by caging them as glycoconjugate prodrugs. Within cancer cells, imidazoquinoline glycoconjugates are activated by hydrolases prior to efflux by ABC transport proteins, where they then elicit tumoricidal effects from the assistance of bystander immune cells, such as tumor-infiltrating lymphocytes and associated macrophages, in local proximity. While this concept of Bystander-Assisted ImmunoTherapy (BAIT) has been established at a molecular level in vitro, tolerability or efficacy of BAIT has not been reported in vivo. Here, we evaluate the MTD and tumor growth delay efficacy of a lead BAIT prodrug (BAIT628) in a male C57BL/6 mouse TRAMP-C2 prostate cancer model to further establish this methodology. Overall, we find that systemic BAIT628 is well tolerated at over 5-fold the dose-limiting inflammatory toxicity of the parent imidazoquinoline (up to 5 mg/mouse/day I.P. for 10 days). Analyzing serum cytokines reveals that IL-10 production, elicited by the mannoside caging group, likely contributes to the enhanced MTD. Using BAIT628 as an in situ vaccination immunotherapy (seven times over 3 weeks) resulted in significant tumor growth delay and increased survival, both alone and in combination with a murinized α-PD-L1 checkpoint blockade. The tumor histology of tumor-infiltrating immune cell subsets (CD4+, CD8+, CD11c+) reveals significant increases in CD11c+ populations, consistent with TLR7/8 agonism. Overall, BAIT628 is well tolerated and exhibits significant efficacy in the TRAMP-C2 model. These results demonstrate how the BAIT approach can optimize imidazoquinolines for in vivo tolerability and subsequent efficacy as cancer immunotherapeutics. Full article
(This article belongs to the Special Issue Advances in Hybrid Anticancer Drugs: Innovations and Therapeutic Potential)
►▼ Show Figures

Figure 1

Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:
 
Displaying articles 1-1
Back to TopTop