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New Anticancer Agents: Design, Synthesis and Evaluation
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New Anticancer Agents: Design, Synthesis and Evaluation

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 16351

Special Issue Editors

Dr. Vadim Pokrovsky

E-Mail Website
Guest Editor
Laboratory of Combined Treatment, N.N. Blokhin National Medical Research Center of Oncology of Ministry of Health of Russian Federation, 115478 Moscow, Russia
Interests: anticancer agents; cancer metabolism; preclinical evaluation of anticancer drugs; animal models of cancer; new targets for cancer therapy
Dr. Mauro Coluccia

E-Mail Website
Guest Editor
Department of Pharmacy-Drug Sciences, University of Bari “Aldo Moro”, Via E. Orabona 4, I-70125 Bari, Italy
Interests: anticancer drugs; targeted anticancer therapeutics; cellular response to anticancer treatment; inflammation and inflammation mediators
Special Issues, Collections and Topics in MDPI journals
Dr. Raffaele Addeo

E-Mail Website
Guest Editor
Medical Oncology Unit, San Giovanni di Dio Hospital, 80027 Frattamaggiore, Naples, Italy
Interests: cancer biology; treatment; tumors; oncology; neurology; cancer therapy; chemotherapy; neuro-oncology; glioblastoma
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

It is a pleasure for me to invite you to contribute to this Special Issue in IJMS to promote the dissemination of knowledge about a wide variety of novel therapies that may enhance the efficacy of anticancer treatment. The design, synthesis and evaluation of new anticancer agents is among the top priority goals of medicinal chemistry, biochemistry and experimental oncology.

Potential contributors are invited to submit papers concerning the recent early-stage development of new therapeutic agents and novel drug targets for the treatment of cancer in any pharmaceutical or related context. Particularly, we welcome non-clinical reports involving new steroid derivatives for prostate cancer treatment, new tyrosine kinases, HDAC inhibitors and other small molecules with prominent anticancer effects, in vitro and in vivo. Novel treatment approaches and new target evaluations are also appreciated. Research areas may include, but are not limited to, the following

  • Rational design of new anticancer agents, including computer-aided drug design and in-silico studies;
  • Screening and early-stage development of small molecules and biologicals;
  • Exploratory and confirmatory non-clinical trials (animal cancer models and in-vitro models);
  • Basic findings about innovative molecularly targeted cancer therapies;
  • Drug delivery and pharmacokinetic studies.

In this Special Issue, we aim to collect outstanding state-of-the-art research and highlight the current progress in anticancer drug development.

Dr. Vadim Pokrovsky
Dr. Mauro Coluccia
Dr. Raffaele Addeo
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

  • medicinal chemistry of anticancer drugs
  • preclinical evaluation
  • cytotoxic effects
  • targets for cancer treatment
  • small molecules for cancer treatment
  • non-clinical anticancer effects
  • biochemistry of tumor cells

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Published Papers (6 papers)

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Research

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14 pages, 4404 KiB  
Article
New Carbonate-Based Materials and Study of Cytotoxic Capacity in Cancer Cells
by Nayara Niza-Pérez, Josefa Quiroz-Troncoso, Nicolás Alegría-Aravena, Santiago Gómez-Ruiz, Diana Díaz-García and Carmen Ramírez-Castillejo
Int. J. Mol. Sci. 2023, 24(6), 5546; https://doi.org/10.3390/ijms24065546 - 14 Mar 2023
Cited by 1 | Viewed by 1897
Abstract
Calcium carbonate, one of the most commonly found biominerals produced by organisms, has shown great potential for the development of systems with biological applications due to its excellent biocompatibility, biodegradability, and simple chemical composition. Here, we focus on the synthesis of various carbonate-based [...] Read more.
Calcium carbonate, one of the most commonly found biominerals produced by organisms, has shown great potential for the development of systems with biological applications due to its excellent biocompatibility, biodegradability, and simple chemical composition. Here, we focus on the synthesis of various carbonate-based materials with vaterite phase control and their subsequent functionalization for applications in treating glioblastoma, one of the most limiting tumors currently without effective treatments. The incorporation of l-cysteine into the systems increased cell selectivity while the incorporation of manganese supplied the materials with cytotoxic capacity. Extensive characterization of the systems by infrared spectroscopy, ultraviolet-visible spectroscopy, X-ray diffraction, X-ray fluorescence, and transmission electron microscopy confirmed the incorporation of the different fragments causing selectivity and cytotoxicity to the systems. To verify their therapeutic activity, the vaterite-based materials were tested in the CT2A cell line (murine glioma) and compared to SKBR3 (breast cancer) and HEK-293T (human kidney) cell lines. These studies on the cytotoxicity of the materials have shown promising results that can encourage future in vivo studies in glioblastoma models. Full article
(This article belongs to the Special Issue New Anticancer Agents: Design, Synthesis and Evaluation)
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16 pages, 1212 KiB  
Communication
Synthesis of 1,4-Dialkoxynaphthalene-Based Imidazolium Salts and Their Cytotoxicity in Cancer Cell Lines
by Haena Lee, Yejin Jeon, Hyejin Moon, Eunjoo H. Lee, Tae Hoon Lee and Hakwon Kim
Int. J. Mol. Sci. 2023, 24(3), 2713; https://doi.org/10.3390/ijms24032713 - 1 Feb 2023
Cited by 3 | Viewed by 1684
Abstract
In this study, we designed and synthesized novel 1,4-dialkoxynaphthalene-2-alkyl imidazolium salt (IMS) derivatives containing both 1,4-dialkoxynaphthalene and imidazole, which are well known as pharmacophores. The cytotoxicities of these newly synthesized IMS derivatives were investigated in order to explore the possibility of using them [...] Read more.
In this study, we designed and synthesized novel 1,4-dialkoxynaphthalene-2-alkyl imidazolium salt (IMS) derivatives containing both 1,4-dialkoxynaphthalene and imidazole, which are well known as pharmacophores. The cytotoxicities of these newly synthesized IMS derivatives were investigated in order to explore the possibility of using them to develop anticancer drugs. It was found that some of the new IMS derivatives showed good cytotoxic activities. In addition, an initial, qualitative structure–activity relationship is presented on the basis of observations of activity changes corresponding to structural changes. Full article
(This article belongs to the Special Issue New Anticancer Agents: Design, Synthesis and Evaluation)
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20 pages, 2203 KiB  
Article
Synthesis and Biological Evaluation of Potential Oncoimmunomodulator Agents
by Raquel Gil-Edo, Sara Espejo, Eva Falomir and Miguel Carda
Int. J. Mol. Sci. 2023, 24(3), 2614; https://doi.org/10.3390/ijms24032614 - 30 Jan 2023
Cited by 5 | Viewed by 2291
Abstract
Fourteen triazole-scaffold derivatives were synthetized and biologically evaluated as potential oncoimmunomodultator agents by targeting both PD-L1 and c-Myc. First, the antiproliferative activity of these molecules on the monocultures of several tumor cell lines (HT-29, A-549, and MCF-7) and on the non-tumor cell line [...] Read more.
Fourteen triazole-scaffold derivatives were synthetized and biologically evaluated as potential oncoimmunomodultator agents by targeting both PD-L1 and c-Myc. First, the antiproliferative activity of these molecules on the monocultures of several tumor cell lines (HT-29, A-549, and MCF-7) and on the non-tumor cell line HEK-293 was studied. Then, the effects on the mentioned biological targets were also evaluated. Finally, the effect on cancer cell viability when the molecules were co-cultured with immune cells (Jurkat T cells or THP-1) was also determined. Compounds bearing a bromoophenyl group were selected because of their excellent results, and their effect on IL-6 secretion was also studied. In conclusion, we found compounds that are capable of downregulating c-Myc, as well as influencing and altering the distribution of PD-L1 in tumor cells; the compounds are thus capable of influencing the behavior of defensive cells towards cancer cells. p-Bromophenyltriazol 3 is the most active of these as a PD-L1 and c-Myc downregulator and as a potential immunomodulator agent. Moreover, it exhibits an interesting action on inflammation-related cytokine IL-6. Full article
(This article belongs to the Special Issue New Anticancer Agents: Design, Synthesis and Evaluation)
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12 pages, 1411 KiB  
Article
Methionine γ-Lyase-Daidzein in Combination with S-Propyl-L-cysteine Sulfoxide as a Targeted Prodrug Enzyme System for Malignant Solid Tumor Xenografts
by Louay Abo Qoura, Elena Morozova, Vitalia Kulikova, Saida Karshieva, Darina Sokolova, Vasiliy Koval, Svetlana Revtovich, Tatyana Demidkina and Vadim S. Pokrovsky
Int. J. Mol. Sci. 2022, 23(19), 12048; https://doi.org/10.3390/ijms231912048 - 10 Oct 2022
Cited by 6 | Viewed by 2674
Abstract
The purpose of this study was to determine the anticancer effect of dipropyl thiosulfinate produced in situ by the pharmacological pair: (1) conjugated with daidzein C115H methionine γ-lyase (EC 4.4.1.11, C115H MGL-Dz) and (2) the substrate, S-propyl-L-cysteine sulfoxide (propiin) against various solid tumor [...] Read more.
The purpose of this study was to determine the anticancer effect of dipropyl thiosulfinate produced in situ by the pharmacological pair: (1) conjugated with daidzein C115H methionine γ-lyase (EC 4.4.1.11, C115H MGL-Dz) and (2) the substrate, S-propyl-L-cysteine sulfoxide (propiin) against various solid tumor types in vitro and in vivo. The MTT test was used to calculate IC50 values for HT29, COLO205 and HCT116 (colon cancer); Panc1 and MIA-PaCa2 (pancreatic cancer); and 22Rv1, DU-145 and PC3 (prostate cancer). The most promising effect for colon cancer cells in vitro was observed in HT29 (IC50 = 6.9 µM). The IC50 values for MIA-PaCa2 and Panc1 were 3.4 and 3.8 µM, respectively. Among prostate cancer cells, 22Rv1 was the most sensitive (IC50 = 5.4 µM). In vivo antitumor activity of the pharmacological pair was studied in HT29, SW620, Panc1, MIA-PaCa2 and 22Rv1 subcutaneous xenografts in BALB/c nude mice. The application of C115H MGL-Dz /propiin demonstrated a significant reduction in the tumor volume of Panc1 (TGI 67%; p = 0.004), MIA-PaCa2 (TGI 50%; p = 0.011), HT29 (TGI 51%; p = 0.04) and 22Rv1 (TGI 70%; p = 0.043) xenografts. The results suggest that the combination of C115H MGL-Dz/propiin is able to suppress tumor growth in vitro and in vivo and the use of this pharmacological pair can be considered as a new strategy for the treatment of solid tumors. Full article
(This article belongs to the Special Issue New Anticancer Agents: Design, Synthesis and Evaluation)
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Review

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34 pages, 12412 KiB  
Review
Inhibitors of NAD+ Production in Cancer Treatment: State of the Art and Perspectives
by Moustafa S. Ghanem, Irene Caffa, Fiammetta Monacelli and Alessio Nencioni
Int. J. Mol. Sci. 2024, 25(4), 2092; https://doi.org/10.3390/ijms25042092 - 8 Feb 2024
Cited by 2 | Viewed by 3305
Abstract
The addiction of tumors to elevated nicotinamide adenine dinucleotide (NAD+) levels is a hallmark of cancer metabolism. Obstructing NAD+ biosynthesis in tumors is a new and promising antineoplastic strategy. Inhibitors developed against nicotinamide phosphoribosyltransferase (NAMPT), the main enzyme in NAD [...] Read more.
The addiction of tumors to elevated nicotinamide adenine dinucleotide (NAD+) levels is a hallmark of cancer metabolism. Obstructing NAD+ biosynthesis in tumors is a new and promising antineoplastic strategy. Inhibitors developed against nicotinamide phosphoribosyltransferase (NAMPT), the main enzyme in NAD+ production from nicotinamide, elicited robust anticancer activity in preclinical models but not in patients, implying that other NAD+-biosynthetic pathways are also active in tumors and provide sufficient NAD+ amounts despite NAMPT obstruction. Recent studies show that NAD+ biosynthesis through the so-called “Preiss-Handler (PH) pathway”, which utilizes nicotinate as a precursor, actively operates in many tumors and accounts for tumor resistance to NAMPT inhibitors. The PH pathway consists of three sequential enzymatic steps that are catalyzed by nicotinate phosphoribosyltransferase (NAPRT), nicotinamide mononucleotide adenylyltransferases (NMNATs), and NAD+ synthetase (NADSYN1). Here, we focus on these enzymes as emerging targets in cancer drug discovery, summarizing their reported inhibitors and describing their current or potential exploitation as anticancer agents. Finally, we also focus on additional NAD+-producing enzymes acting in alternative NAD+-producing routes that could also be relevant in tumors and thus become viable targets for drug discovery. Full article
(This article belongs to the Special Issue New Anticancer Agents: Design, Synthesis and Evaluation)
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24 pages, 12655 KiB  
Review
4-Thiazolidinone-Bearing Hybrid Molecules in Anticancer Drug Design
by Piotr Roszczenko, Serhii Holota, Olga Klaudia Szewczyk, Rostyslav Dudchak, Krzysztof Bielawski, Anna Bielawska and Roman Lesyk
Int. J. Mol. Sci. 2022, 23(21), 13135; https://doi.org/10.3390/ijms232113135 - 28 Oct 2022
Cited by 39 | Viewed by 3365
Abstract
Oncological diseases have currently reached an epidemic scale, especially in industrialized countries. Such a situation has prompted complex studies in medicinal chemistry focused on the research and development of novel effective anticancer drugs. In this review, the data concerning new 4-thiazolidinone-bearing hybrid molecules [...] Read more.
Oncological diseases have currently reached an epidemic scale, especially in industrialized countries. Such a situation has prompted complex studies in medicinal chemistry focused on the research and development of novel effective anticancer drugs. In this review, the data concerning new 4-thiazolidinone-bearing hybrid molecules with potential anticancer activity reported during the period from the years 2017–2022 are summarized. The main emphasis is on the application of molecular hybridization methodologies and strategies in the design of small molecules as anticancer agents. Based on the analyzed data, it was observed that the main directions in this field are the hybridization of scaffolds, the hybrid-pharmacophore approach, and the analogue-based drug design of 4-thiazolidinone cores with early approved drugs, natural compounds, and privileged heterocyclic scaffolds. The mentioned design approaches are effective tools/sources for the generation of hit/lead compounds with anticancer activity and will be relevant to future studies. Full article
(This article belongs to the Special Issue New Anticancer Agents: Design, Synthesis and Evaluation)
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