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Advances in the Development of Anticancer Drugs
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Advances in the Development of Anticancer Drugs

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

Deadline for manuscript submissions: closed (30 November 2023) | Viewed by 10745

Special Issue Editors

Prof. Dr. Jean Fotie

E-Mail Website
Guest Editor
Department of Chemistry and Physics, Southeastern Louisiana University, SLU 10878, Hammond, LA 70402-0878, USA
Interests: green and sustainable chemistry; catalysis; medicinal chemistry; silicon-based amino acids; skin cancer
Dr. Jean Christopher Chamcheu

E-Mail Website
Guest Editor
Department of Biological Sciences and Chemistry, College of Sciences and Engineering, Southern University and A&M College, Baton Rouge, LA 70807, USA
Interests: skin health and diseases; carcinogenesis; inflammation; dermatology; psoriasis; atopic dermatitis; bioactive natural products; antioxidants; polyphenols; flavonoids; tissue engineering; signaling pathways; pharmacology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Recent studies have indicated that cancer is one of the leading causes of death worldwide, with the number of new cancer cases per year expected to rise to about 30 million by 2040, with more than half of these cases resulting in deaths. Furthermore, unlike many other ailments, cancers are more prevalent in countries where populations generally have higher life expectancy, better education, and an optimal standard of living. Despite significant advances in prevention, diagnosis, and treatment, current therapeutic methods are often hampered by the lack of selectivity and a high level of toxicity. As a result, there is an urgent need for the development of safe, selective, and more efficient chemotherapeutic agents. One approach toward solving this situation is the introduction of new chemotherapeutic molecules into the anticancer drug pipeline. The current Special Issue invites research articles, reviews, and expert opinion reviews on recent advancements in anticancer drug design and development. This includes but is not limited to:

  • Identification of small organic molecules as new anticancer lead compounds;
  • Design, synthesis, and evaluation of new cancer therapeutic agents;
  • Structure–activity relationship investigation;
  • In silico, in vitro,and in vivo studies;
  • Potential therapeutic targets and molecular mechanism.

Prof. Dr. Jean Fotie
Dr. Jean Christopher Chamcheu
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. 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

  • anticancer

Published Papers (6 papers)

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Editorial

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3 pages, 173 KiB  
Editorial
Editorial for the Special Issue “Advances in the Development of Anticancer Drugs”
by Jean Fotie
Int. J. Mol. Sci. 2024, 25(1), 641; https://doi.org/10.3390/ijms25010641 - 04 Jan 2024
Viewed by 679
Abstract
As mortality rates for other leading causes of death, such as stroke and coronary heart disease, decline in many parts of the world, cancer is becoming the leading cause of death worldwide, with the number of yearly new cases expected to rise to [...] Read more.
As mortality rates for other leading causes of death, such as stroke and coronary heart disease, decline in many parts of the world, cancer is becoming the leading cause of death worldwide, with the number of yearly new cases expected to rise to about 30 million by 2040 [...] Full article
(This article belongs to the Special Issue Advances in the Development of Anticancer Drugs)

Research

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11 pages, 1941 KiB  
Communication
Study of Lipophilicity and ADME Properties of 1,9-Diazaphenothiazines with Anticancer Action
by Beata Morak-Młodawska, Małgorzata Jeleń, Emilia Martula and Rafał Korlacki
Int. J. Mol. Sci. 2023, 24(8), 6970; https://doi.org/10.3390/ijms24086970 - 09 Apr 2023
Cited by 8 | Viewed by 1836
Abstract
Lipophilicity is one of the key properties of a potential drug that determines the solubility, the ability to penetrate through cell barriers, and transport to the molecular target. It affects pharmacokinetic processes such as adsorption, distribution, metabolism, excretion (ADME). The 10-substituted 1,9-diazaphenothiazines show [...] Read more.
Lipophilicity is one of the key properties of a potential drug that determines the solubility, the ability to penetrate through cell barriers, and transport to the molecular target. It affects pharmacokinetic processes such as adsorption, distribution, metabolism, excretion (ADME). The 10-substituted 1,9-diazaphenothiazines show promising if not impressive in vitro anticancer potential, which is associated with the activation of the mitochondrial apoptosis pathway connected with to induction BAX, forming a channel in MOMP and releasing cytochrome c for the activation of caspases 9 and 3. In this publication, the lipophilicity of previously obtained 1,9-diazaphenothiazines was determined theoretically using various computer programs and experimentally using reverse-phase thin-layer chromatography (RP-TLC) and a standard curve. The study presents other physicochemical, pharmacokinetic, and toxicological properties affecting the bioavailability of the test compounds. ADME analysis was determined in silico using the SwissADME server. Molecular targets studies were identified in silico using the SwissTargetPrediction server. Lipinski’s rule of five, Ghose’s, and Veber’s rules were checked for the tested compounds, confirming their bioavailability. Full article
(This article belongs to the Special Issue Advances in the Development of Anticancer Drugs)
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19 pages, 2926 KiB  
Article
Ruthenium Complexes with Protic Ligands: Influence of the Position of OH Groups and π Expansion on Luminescence and Photocytotoxicity
by Olaitan E. Oladipupo, Meredith C. Prescott, Emily R. Blevins, Jessica L. Gray, Colin G. Cameron, Fengrui Qu, Nicholas A. Ward, Abigail L. Pierce, Elizabeth R. Collinson, James Fletcher Hall, Seungjo Park, Yonghyun Kim, Sherri A. McFarland, Igor Fedin and Elizabeth T. Papish
Int. J. Mol. Sci. 2023, 24(6), 5980; https://doi.org/10.3390/ijms24065980 - 22 Mar 2023
Cited by 3 | Viewed by 1904
Abstract
Protic ruthenium complexes using the dihydroxybipyridine (dhbp) ligand combined with a spectator ligand (N,N = bpy, phen, dop, Bphen) have been studied for their potential activity vs. cancer cells and their photophysical luminescent properties. These complexes vary in the extent of π expansion [...] Read more.
Protic ruthenium complexes using the dihydroxybipyridine (dhbp) ligand combined with a spectator ligand (N,N = bpy, phen, dop, Bphen) have been studied for their potential activity vs. cancer cells and their photophysical luminescent properties. These complexes vary in the extent of π expansion and the use of proximal (6,6′-dhbp) or distal (4,4′-dhbp) hydroxy groups. Eight complexes are studied herein as the acidic (OH bearing) form, [(N,N)2Ru(n,n′-dhbp)]Cl2, or as the doubly deprotonated (O− bearing) form. Thus, the presence of these two protonation states gives 16 complexes that have been isolated and studied. Complex 7A, [(dop)2Ru(4,4′-dhbp)]Cl2, has been recently synthesized and characterized spectroscopically and by X-ray crystallography. The deprotonated forms of three complexes are also reported herein for the first time. The other complexes studied have been synthesized previously. Three complexes are light-activated and exhibit photocytotoxicity. The log(Do/w) values of the complexes are used herein to correlate photocytotoxicity with improved cellular uptake. For Ru complexes 1–4 bearing the 6,6′-dhbp ligand, photoluminescence studies (all in deaerated acetonitrile) have revealed that steric strain leads to photodissociation which tends to reduce photoluminescent lifetimes and quantum yields in both protonation states. For Ru complexes 5–8 bearing the 4,4′-dhbp ligand, the deprotonated Ru complexes (5B–8B) have low photoluminescent lifetimes and quantum yields due to quenching that is proposed to involve the 3LLCT excited state and charge transfer from the [O2-bpy]2− ligand to the N,N spectator ligand. The protonated OH bearing 4,4′-dhbp Ru complexes (5A–8A) have long luminescence lifetimes which increase with increasing π expansion on the N,N spectator ligand. The Bphen complex, 8A, has the longest lifetime of the series at 3.45 μs and a photoluminescence quantum yield of 18.7%. This Ru complex also exhibits the best photocytotoxicity of the series. A long luminescence lifetime is correlated with greater singlet oxygen quantum yields because the triplet excited state is presumably long-lived enough to interact with 3O2 to yield 1O2. Full article
(This article belongs to the Special Issue Advances in the Development of Anticancer Drugs)
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Review

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53 pages, 4560 KiB  
Review
The Fundamental Role of Oxime and Oxime Ether Moieties in Improving the Physicochemical and Anticancer Properties of Structurally Diverse Scaffolds
by Jean Fotie, Caitlyn M. Matherne, Jasmine B. Mather, Jordan E. Wroblewski, Khaitlynn Johnson, Lara G. Boudreaux and Alba A. Perez
Int. J. Mol. Sci. 2023, 24(23), 16854; https://doi.org/10.3390/ijms242316854 - 28 Nov 2023
Cited by 1 | Viewed by 918
Abstract
The present review explores the critical role of oxime and oxime ether moieties in enhancing the physicochemical and anticancer properties of structurally diverse molecular frameworks. Specific examples are carefully selected to illustrate the distinct contributions of these functional groups to general strategies for [...] Read more.
The present review explores the critical role of oxime and oxime ether moieties in enhancing the physicochemical and anticancer properties of structurally diverse molecular frameworks. Specific examples are carefully selected to illustrate the distinct contributions of these functional groups to general strategies for molecular design, modulation of biological activities, computational modeling, and structure–activity relationship studies. An extensive literature search was conducted across three databases, including PubMed, Google Scholar, and Scifinder, enabling us to create one of the most comprehensive overviews of how oximes and oxime ethers impact antitumor activities within a wide range of structural frameworks. This search focused on various combinations of keywords or their synonyms, related to the anticancer activity of oximes and oxime ethers, structure–activity relationships, mechanism of action, as well as molecular dynamics and docking studies. Each article was evaluated based on its scientific merit and the depth of the study, resulting in 268 cited references and more than 336 illustrative chemical structures carefully selected to support this analysis. As many previous reviews focus on one subclass of this extensive family of compounds, this report represents one of the rare and fully comprehensive assessments of the anticancer potential of this group of molecules across diverse molecular scaffolds. Full article
(This article belongs to the Special Issue Advances in the Development of Anticancer Drugs)
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28 pages, 6253 KiB  
Review
Computational Approaches Drive Developments in Immune-Oncology Therapies for PD-1/PD-L1 Immune Checkpoint Inhibitors
by Patrícia S. Sobral, Vanessa C. C. Luz, João M. G. C. F. Almeida, Paula A. Videira and Florbela Pereira
Int. J. Mol. Sci. 2023, 24(6), 5908; https://doi.org/10.3390/ijms24065908 - 21 Mar 2023
Cited by 4 | Viewed by 2778
Abstract
Computational approaches in immune-oncology therapies focus on using data-driven methods to identify potential immune targets and develop novel drug candidates. In particular, the search for PD-1/PD-L1 immune checkpoint inhibitors (ICIs) has enlivened the field, leveraging the use of cheminformatics and bioinformatics tools to [...] Read more.
Computational approaches in immune-oncology therapies focus on using data-driven methods to identify potential immune targets and develop novel drug candidates. In particular, the search for PD-1/PD-L1 immune checkpoint inhibitors (ICIs) has enlivened the field, leveraging the use of cheminformatics and bioinformatics tools to analyze large datasets of molecules, gene expression and protein–protein interactions. Up to now, there is still an unmet clinical need for improved ICIs and reliable predictive biomarkers. In this review, we highlight the computational methodologies applied to discovering and developing PD-1/PD-L1 ICIs for improved cancer immunotherapies with a greater focus in the last five years. The use of computer-aided drug design structure- and ligand-based virtual screening processes, molecular docking, homology modeling and molecular dynamics simulations methodologies essential for successful drug discovery campaigns focusing on antibodies, peptides or small-molecule ICIs are addressed. A list of recent databases and web tools used in the context of cancer and immunotherapy has been compilated and made available, namely regarding a general scope, cancer and immunology. In summary, computational approaches have become valuable tools for discovering and developing ICIs. Despite significant progress, there is still a need for improved ICIs and biomarkers, and recent databases and web tools have been compiled to aid in this pursuit. Full article
(This article belongs to the Special Issue Advances in the Development of Anticancer Drugs)
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18 pages, 2091 KiB  
Review
A Brief Review on Chemoresistance; Targeting Cancer Stem Cells as an Alternative Approach
by Belén Toledo, Aitor González-Titos, Pablo Hernández-Camarero and Macarena Perán
Int. J. Mol. Sci. 2023, 24(5), 4487; https://doi.org/10.3390/ijms24054487 - 24 Feb 2023
Cited by 4 | Viewed by 2029
Abstract
The acquisition of resistance to traditional chemotherapy and the chemoresistant metastatic relapse of minimal residual disease both play a key role in the treatment failure and poor prognosis of cancer. Understanding how cancer cells overcome chemotherapy-induced cell death is critical to improve patient [...] Read more.
The acquisition of resistance to traditional chemotherapy and the chemoresistant metastatic relapse of minimal residual disease both play a key role in the treatment failure and poor prognosis of cancer. Understanding how cancer cells overcome chemotherapy-induced cell death is critical to improve patient survival rate. Here, we briefly describe the technical approach directed at obtaining chemoresistant cell lines and we will focus on the main defense mechanisms against common chemotherapy triggers by tumor cells. Such as, the alteration of drug influx/efflux, the enhancement of drug metabolic neutralization, the improvement of DNA-repair mechanisms, the inhibition of apoptosis-related cell death, and the role of p53 and reactive oxygen species (ROS) levels in chemoresistance. Furthermore, we will focus on cancer stem cells (CSCs), the cell population that subsists after chemotherapy, increasing drug resistance by different processes such as epithelial-mesenchymal transition (EMT), an enhanced DNA repair machinery, and the capacity to avoid apoptosis mediated by BCL2 family proteins, such as BCL-XL, and the flexibility of their metabolism. Finally, we will review the latest approaches aimed at decreasing CSCs. Nevertheless, the development of long-term therapies to manage and control CSCs populations within the tumors is still necessary. Full article
(This article belongs to the Special Issue Advances in the Development of Anticancer Drugs)
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