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Applied Sciences
Special Issues
Anticancer Drugs Activity and Underlying Mechanisms
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Anticancer Drugs Activity and Underlying Mechanisms

A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Applied Biosciences and Bioengineering".

Deadline for manuscript submissions: closed (30 April 2021) | Viewed by 34927

Printed Edition Available!
A printed edition of this Special Issue is available here.

Special Issue Editor

Prof. Dr. Domenico Iacopetta

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Guest Editor
Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via Pietro Bucci, 87036 Arcavacata di Rende, Italy
Interests: food; medicinal chemistry; bioactive products; nutraceuticals; phytochemicals; natural products extraction and isolation; antioxidants; anti-inflammatory; antimicrobials enzyme inhibition; cancer; cell biology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

You are cordially invited to contribute to this Special Issue entitled “Anticancer Drugs Activity and Underlying Mechanisms”. As you know, cancer is a multifactorial disease and its onset and progression are very complex. Even though prevention, early diagnoses, and new therapies have been implemented, cancer is still the second leading cause of death worldwide. The continuous fight against cancer has led several researchers to develop new, more powerful, and safer molecules or repurpose old ones with unknown antitumor activities. A trend to customize the therapy has been recorded, together with the need to design and study drugs selectively targeting a cell component, with few toxic effects. However, clinical experiences have reinforced the idea that targeting a single cell component may not be the real mechanism by which drugs produce the desired effect; indeed, cells could become resistant to the treatment, for instance, activating compensatory pathways. Thus, the multi-target drugs concept and the individuation of the underlying mechanisms represent rich and fertile fields for drug research and development. The major issue of the emergence of multidrug resistance and relapse has been faced using, for instance, genomic/proteomic profiling technologies and selective molecular targeted therapies. This Special Issue addresses several old chemotherapeutic drugs or newer ones, whose cellular mechanisms are not well explicated and detailed. Original research papers or review articles on the design, synthesis, and evaluation of drugs or metal complexes targeting biomolecules such as tubulin and topoisomerase are very welcome.

Dr. Domenico Iacopetta
Guest Editor

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-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Applied Sciences 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 2400 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

  • Design and synthesis of new antitumor drugs
  • Natural or chemically modified drugs
  • Carbazoles derivatives
  • Metal complexes
  • Human topoisomerases inhibitors
  • Drugs interfering with cytoskeleton dynamics
  • Drug repurposing
  • Kinases inhibitors
  • Intercalating agents
  • Mitochondria-targeting drugs
  • Steroid-hormones-targeting drugs

Published Papers (11 papers)

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Editorial

Jump to: Research, Review, Other

5 pages, 208 KiB  
Editorial
Special Issue on “Anticancer Drugs Activity and Underlying Mechanisms”
by Domenico Iacopetta
Appl. Sci. 2021, 11(17), 8169; https://doi.org/10.3390/app11178169 - 03 Sep 2021
Cited by 2 | Viewed by 1052
Abstract
Cancer is a reputed non-communicable disease, namely a non-transmittable illness affecting humankind, which represents a major public health issue and is one of the leading causes of death worldwide [...] Full article
(This article belongs to the Special Issue Anticancer Drugs Activity and Underlying Mechanisms)

Research

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15 pages, 3912 KiB  
Article
Simple Thalidomide Analogs in Melanoma: Synthesis and Biological Activity
by Alexia Barbarossa, Alessia Catalano, Jessica Ceramella, Alessia Carocci, Domenico Iacopetta, Camillo Rosano, Carlo Franchini and Maria Stefania Sinicropi
Appl. Sci. 2021, 11(13), 5823; https://doi.org/10.3390/app11135823 - 23 Jun 2021
Cited by 6 | Viewed by 2385
Abstract
Thalidomide is an old well-known drug that is still of clinical interest, despite its teratogenic activities, due to its antiangiogenic and immunomodulatory properties. Therefore, efforts to design safer and effective thalidomide analogs are continually ongoing. Research studies on thalidomide analogs have revealed that [...] Read more.
Thalidomide is an old well-known drug that is still of clinical interest, despite its teratogenic activities, due to its antiangiogenic and immunomodulatory properties. Therefore, efforts to design safer and effective thalidomide analogs are continually ongoing. Research studies on thalidomide analogs have revealed that the phthalimide ring system is an essential pharmacophoric fragment; thus, many phthalimidic compounds have been synthesized and evaluated as anticancer drug candidates. In this study, a panel of selected in vitro assays, performed on a small series of phthalimide derivatives, allowed us to characterize compound 2k as a good anticancer agent, acting on A2058 melanoma cell line, which causes cell death by apoptosis due to its capability to inhibit tubulin polymerization. The obtained data were confirmed by in silico assays. No cytotoxic effects on normal cells have been detected for this compound that proves to be a valid candidate for further investigations to achieve new insights on possible mechanism of action of this class of compounds as anticancer drugs. Full article
(This article belongs to the Special Issue Anticancer Drugs Activity and Underlying Mechanisms)
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13 pages, 4283 KiB  
Article
N-Heterocyclic Carbene-Gold(I) Complexes Targeting Actin Polymerization
by Domenico Iacopetta, Jessica Ceramella, Camillo Rosano, Annaluisa Mariconda, Michele Pellegrino, Marco Sirignano, Carmela Saturnino, Alessia Catalano, Stefano Aquaro, Pasquale Longo and Maria Stefania Sinicropi
Appl. Sci. 2021, 11(12), 5626; https://doi.org/10.3390/app11125626 - 18 Jun 2021
Cited by 17 | Viewed by 2301
Abstract
Transition metal complexes are attracting attention because of their various chemical and biological properties. In particular, the NHC-gold complexes represent a productive field of research in medicinal chemistry, mostly as anticancer tools, displaying a broad range of targets. In addition to the already [...] Read more.
Transition metal complexes are attracting attention because of their various chemical and biological properties. In particular, the NHC-gold complexes represent a productive field of research in medicinal chemistry, mostly as anticancer tools, displaying a broad range of targets. In addition to the already known biological targets, recently, an important activity in the organization of the cell cytoskeleton was discovered. In this paper, we demonstrated that two NHC-gold complexes (namely AuL4 and AuL7) possessing good anticancer activity and multi-target properties, as stated in our previous studies, play a major role in regulating the actin polymerization, by the means of in silico and in vitro assays. Using immunofluorescence and direct enzymatic assays, we proved that both the complexes inhibited the actin polymerization reaction without promoting the depolymerization of actin filaments. Our outcomes may contribute toward deepening the knowledge of NHC-gold complexes, with the objective of producing more effective and safer drugs for treating cancer diseases. Full article
(This article belongs to the Special Issue Anticancer Drugs Activity and Underlying Mechanisms)
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Graphical abstract

14 pages, 9245 KiB  
Article
Improved Anticancer Activity of the Malloapelta B-Nanoliposomal Complex against Lung Carcinoma
by Thi Thao Do, Thi Nga Nguyen, Thi Phuong Do, Thi Cuc Nguyen, Ha Phuong Trieu, Phuong Thi Thu Vu and Tuan Anh Hoang Le
Appl. Sci. 2020, 10(22), 8148; https://doi.org/10.3390/app10228148 - 17 Nov 2020
Cited by 1 | Viewed by 1966
Abstract
Previous studies regarding malloapelta B (malB), a natural compound isolated from the Vietnamese medicinal plant, showed a strong NF-κB inhibitory effect, making it a promising source for the development of novel anticancer drugs. However, similar to many other natural compounds from plants, malB [...] Read more.
Previous studies regarding malloapelta B (malB), a natural compound isolated from the Vietnamese medicinal plant, showed a strong NF-κB inhibitory effect, making it a promising source for the development of novel anticancer drugs. However, similar to many other natural compounds from plants, malB has several disadvantages for clinical applications, including high toxicity and low solubility. To improve its bioavailability, malB was conjugated into nanoliposomes, which are ideal drug carriers. The formulations with 1,2-dipalmitoyl-sn-glycero-3-phosphocholine, mPEG-cholesterol, malB, with or without cholesterol exhibited nanoliposomes with an average diameter of approximately 76.98 nm, PDI of 0.28, zeta potential of −5.53 mV, and the highest encapsulation efficiency of 78.73% ± 9.5%. These malB-nanoliposomes inhibited the survival of all lung cancer cell lines examined with IC50 values ranging from 11.86 to 13.12 µM. Moreover, malB-nanoliposomes showed stronger inhibition of A549 colony-forming activity compared to that of the free compound. The effects of malB and its nanoliposomal formulation may be mediated through activation of apoptosis by the significant induction of caspase 3 activity. The nanoliposomal formulations also showed potential to inhibit tumor growth (37.03%) and prolong survival (32.20 days) of tumor-bearing mice compared with the unloaded drug (p < 0.05). The improved antitumor activity of malB-nanoliposomes suggests their promising clinical applications. Full article
(This article belongs to the Special Issue Anticancer Drugs Activity and Underlying Mechanisms)
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16 pages, 3769 KiB  
Article
The Cytotoxic Effect of Newly Synthesized Ferrocenes against Cervical Carcinoma Cells Alone and in Combination with Radiotherapy
by Hana Skoupilova, Vladimir Rak, Jiri Pinkas, Jindrich Karban and Roman Hrstka
Appl. Sci. 2020, 10(11), 3728; https://doi.org/10.3390/app10113728 - 28 May 2020
Cited by 4 | Viewed by 2035
Abstract
Cervical cancer is one of the most common types of cancer in women, with approximately 500,000 new cases and 250,000 deaths every year. Radiotherapy combined with chemotherapy represents the treatment of choice for advanced cervical carcinomas. The role of the chemotherapy is to [...] Read more.
Cervical cancer is one of the most common types of cancer in women, with approximately 500,000 new cases and 250,000 deaths every year. Radiotherapy combined with chemotherapy represents the treatment of choice for advanced cervical carcinomas. The role of the chemotherapy is to increase the sensitivity of the cancer cells to irradiation. Cisplatin, the most commonly used drug for this purpose, has its limitations. Thus, we used a family of ferrocene derivatives (in addition, one new species was prepared using standard Schlenk techniques) and studied their effects on cervical cancer cells alone and in combination with irradiation. We applied colorimetric assay to determine the cytotoxicity of the compounds; flow cytometry to analyze the production of reactive oxygen species (ROS), cell cycle, and mitochondrial membrane potential (MMP); immunochemistry to study protein expression; and colony forming assay to evaluate changes in radiosensitivity. Treatment with ferrocenes exhibited significant cytotoxicity against cervical cancer cells, associated with increasing ROS production and MMP changes, suggesting the induction of apoptosis. The combined activity of ferrocenes and ionizing radiation highlighted ferrocenes as potential radiosensitizing drugs, while their higher single-agent toxicity in comparison with routinely used cisplatin could also be promising. Our results demonstrate antitumor activity of several tested ferrocenes both alone and in combination with radiotherapy. Full article
(This article belongs to the Special Issue Anticancer Drugs Activity and Underlying Mechanisms)
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Review

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15 pages, 2607 KiB  
Review
Gold Derivatives Development as Prospective Anticancer Drugs for Breast Cancer Treatment
by Ileana Ielo, Domenico Iacopetta, Carmela Saturnino, Pasquale Longo, Maurilio Galletta, Dario Drommi, Giuseppe Rosace, Maria Stefania Sinicropi and Maria Rosaria Plutino
Appl. Sci. 2021, 11(5), 2089; https://doi.org/10.3390/app11052089 - 26 Feb 2021
Cited by 11 | Viewed by 2266
Abstract
Commonly used anticancer drugs are cisplatin and other platinum-based drugs. However, the use of these drugs in chemotherapy causes numerous side effects and the onset of frequent drug resistance phenomena. This review summarizes the most recent results on the gold derivatives used [...] Read more.
Commonly used anticancer drugs are cisplatin and other platinum-based drugs. However, the use of these drugs in chemotherapy causes numerous side effects and the onset of frequent drug resistance phenomena. This review summarizes the most recent results on the gold derivatives used for their significant inhibitory effects on the in vitro proliferation of breast cancer cell models and for the consequences deriving from morphological changes in the same cells. In particular, the study discusses the antitumor activity of gold nanoparticles, gold (I) and (III) compounds, gold complexes and carbene-based gold complexes, compared with cisplatin. The results of screening studies of cytotoxicity and antitumor activity for the gold derivatives show that the death of cancer cells can occur intrinsically by apoptosis. Recent research has shown that gold (III) compounds with square planar geometries, such as that of cisplatin, can intercalate the DNA and provide novel anticancer agents. The gold derivatives described can make an important contribution to expanding the knowledge of medicinal bioorganometallic chemistry and broadening the range of anticancer agents available, offering improved characteristics, such as increased activity and/or selectivity, and paving the way for further discoveries and applications. Full article
(This article belongs to the Special Issue Anticancer Drugs Activity and Underlying Mechanisms)
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20 pages, 9181 KiB  
Review
Schiff Bases: Interesting Scaffolds with Promising Antitumoral Properties
by Domenico Iacopetta, Jessica Ceramella, Alessia Catalano, Carmela Saturnino, Maria Grazia Bonomo, Carlo Franchini and Maria Stefania Sinicropi
Appl. Sci. 2021, 11(4), 1877; https://doi.org/10.3390/app11041877 - 20 Feb 2021
Cited by 56 | Viewed by 4443
Abstract
Schiff bases, named after Hugo Schiff, are highly reactive organic compounds broadly used as pigments and dyes, catalysts, intermediates in organic synthesis, and polymer stabilizers. Lots of Schiff bases are described in the literature for various biological activities, including antimalarial, antibacterial, antifungal, anti-inflammatory, [...] Read more.
Schiff bases, named after Hugo Schiff, are highly reactive organic compounds broadly used as pigments and dyes, catalysts, intermediates in organic synthesis, and polymer stabilizers. Lots of Schiff bases are described in the literature for various biological activities, including antimalarial, antibacterial, antifungal, anti-inflammatory, and antiviral. Schiff bases are also known for their ability to form complexes with several metals. Very often, complexes of Schiff bases with metals and Schiff bases alone have demonstrated interesting antitumor activity. Given the innumerable vastness of data regarding antitumor activity of all these compounds, we focused our attention on mono- and bis-Schiff bases alone as antitumor agents. We will highlight the most significant examples of compounds belonging to this class reported in the literature. Full article
(This article belongs to the Special Issue Anticancer Drugs Activity and Underlying Mechanisms)
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17 pages, 4176 KiB  
Review
Diarylureas as Antitumor Agents
by Alessia Catalano, Domenico Iacopetta, Maria Stefania Sinicropi and Carlo Franchini
Appl. Sci. 2021, 11(1), 374; https://doi.org/10.3390/app11010374 - 02 Jan 2021
Cited by 38 | Viewed by 3903
Abstract
The diarylurea is a scaffold of great importance in medicinal chemistry as it is present in numerous heterocyclic compounds with antithrombotic, antimalarial, antibacterial, and anti-inflammatory properties. Some diarylureas, serine-threonine kinase or tyrosine kinase inhibitors, were recently reported in literature. The first to come [...] Read more.
The diarylurea is a scaffold of great importance in medicinal chemistry as it is present in numerous heterocyclic compounds with antithrombotic, antimalarial, antibacterial, and anti-inflammatory properties. Some diarylureas, serine-threonine kinase or tyrosine kinase inhibitors, were recently reported in literature. The first to come into the market as an anticancer agent was sorafenib, followed by some others. In this review, we survey progress over the past 10 years in the development of new diarylureas as anticancer agents. Full article
(This article belongs to the Special Issue Anticancer Drugs Activity and Underlying Mechanisms)
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13 pages, 1109 KiB  
Review
An Updated Review of Smac Mimetics, LCL161, Birinapant, and GDC-0152 in Cancer Treatment
by Yung-Chieh Chang and Chun Hei Antonio Cheung
Appl. Sci. 2021, 11(1), 335; https://doi.org/10.3390/app11010335 - 31 Dec 2020
Cited by 17 | Viewed by 6427
Abstract
Inhibitor of apoptosis proteins (IAPs) are suggested as therapeutic targets for cancer treatment. Smac/DIABLO is a natural IAP antagonist in cells; therefore, Smac mimetics have been developed for cancer treatment in the past decade. In this article, we review the anti-cancer potency and [...] Read more.
Inhibitor of apoptosis proteins (IAPs) are suggested as therapeutic targets for cancer treatment. Smac/DIABLO is a natural IAP antagonist in cells; therefore, Smac mimetics have been developed for cancer treatment in the past decade. In this article, we review the anti-cancer potency and novel molecular targets of LCL161, birinapant, and GDC-0152. Preclinical studies demonstrated that Smac mimetics not only induce apoptosis but also arrest cell cycle, induce necroptosis, and induce immune storm in vitro and in vivo. The safety and tolerance of Smac mimetics are evaluated in phase 1 and phase 2 clinical trials. In addition, the combination of Smac mimetics and chemotherapeutic compounds was reported to improve anti-cancer effects. Interestingly, the novel anti-cancer molecular mechanism of action of Smac mimetics was reported in recent studies, suggesting that many unknown functions of Smac mimetics still need to be revealed. Exploring these currently unknown signaling pathways is important to provide hints for the modification and combination therapy of further compounds. Full article
(This article belongs to the Special Issue Anticancer Drugs Activity and Underlying Mechanisms)
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18 pages, 258 KiB  
Review
Integration of Molecular Docking and In Vitro Studies: A Powerful Approach for Drug Discovery in Breast Cancer
by Claudia Cava and Isabella Castiglioni
Appl. Sci. 2020, 10(19), 6981; https://doi.org/10.3390/app10196981 - 06 Oct 2020
Cited by 19 | Viewed by 4697
Abstract
Molecular docking in the pharmaceutical industry is a powerful in silico approach for discovering novel therapies for unmet medical needs predicting drug–target interactions. It not only provides binding affinity between drugs and targets at the atomic level, but also elucidates the fundamental pharmacological [...] Read more.
Molecular docking in the pharmaceutical industry is a powerful in silico approach for discovering novel therapies for unmet medical needs predicting drug–target interactions. It not only provides binding affinity between drugs and targets at the atomic level, but also elucidates the fundamental pharmacological properties of specific drugs. The purpose of this review was to illustrate newer and emergent uses of docking when combined with in vitro techniques for drug discovery in metastatic breast cancer. We grouped the selected articles into five main categories; namely, systematic repositioning of drugs, natural drugs, new synthesized molecules, combinations of drugs, and drug latentiation. We focused on new promising drugs that have a good affinity with their targets, thus inducing a favorable biological response. This review suggests that the integration of molecular docking and in vitro studies can accelerate cancer drug discovery showing a good consistency of the results between the two approaches. Full article
(This article belongs to the Special Issue Anticancer Drugs Activity and Underlying Mechanisms)

Other

6 pages, 507 KiB  
Hypothesis
Ibrutinib Could Suppress CA-125 in Ovarian Cancer: A Hypothesis
by Julian Matthias Metzler, Daniel Fink and Patrick Imesch
Appl. Sci. 2021, 11(1), 222; https://doi.org/10.3390/app11010222 - 28 Dec 2020
Cited by 2 | Viewed by 2388
Abstract
Ibrutinib is a small-molecule inhibitor of Bruton’s tyrosine kinase, an enzyme central in B cell development. It is indicated as a therapy for certain hematological diseases such as chronic lymphocytic leukemia (CLL), but also exerts off-target effects on several receptors and kinases. In [...] Read more.
Ibrutinib is a small-molecule inhibitor of Bruton’s tyrosine kinase, an enzyme central in B cell development. It is indicated as a therapy for certain hematological diseases such as chronic lymphocytic leukemia (CLL), but also exerts off-target effects on several receptors and kinases. In this paper, we hypothesize that ibrutinib may suppress the tumor marker CA-125 in ovarian cancer. The hypothesis is based on an observation of CA-125 normalization in a patient with low-grade serous ovarian cancer who received ibrutinib for concurrent CLL. We propose a mechanistic model explaining this possible drug effect as a foundation for further research. Full article
(This article belongs to the Special Issue Anticancer Drugs Activity and Underlying Mechanisms)
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