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Novel Anti-proliferative Agents, 2nd Edition
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Novel Anti-proliferative Agents, 2nd Edition

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

Deadline for manuscript submissions: closed (31 January 2025) | Viewed by 8043

Special Issue Editor

Prof. Dr. Valentina Onnis

E-Mail Website1 Website2
Guest Editor
Department of Life and Environmental Sciences, Unit of Pharmaceutical, Pharmacological and Nutraceutical Sciences, University of Cagliari, University Campus, I-09042 Monserrato, Italy
Interests: medicinal chemistry; nitrogen heterocycles; antiproliferative compounds; enzyme inhibitors
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Cancer is one of the most widely spread and complex forms of disease, as cancer cells are distinguished from healthy cells due to their altered proliferation and survival. In the past three decades, the National Cancer Institute (NCI) alone has screened millions of small molecules for potential anticancer activity. Despite a number of conventional cytotoxic approaches having been developed, their limited effectiveness, in accordance with the heterogeneity of cancer cells, prompts the constant search for novel natural or synthetic compounds with properties involved in growth inhibition or tumor cell activity reduction.

This Special Issue of Pharmaceuticals invites both reviews and original articles regarding basic, preclinical and clinical studies on antiproliferative chemical entities.

I look forward to receiving your contributions.

Prof. Dr. Valentina Onnis
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

  • medicinal chemistry
  • drug discovery
  • natural compounds
  • synthetic compounds
  • organic synthesis
  • bioactivity
  • anticancer drugs
  • antiproliferative activity

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Published Papers (5 papers)

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Research

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16 pages, 2523 KiB  
Article
Antiproliferative Effect of 7-Ketositosterol in Breast and Liver Cancer Cells: Possible Impact on Ceramide, Extracellular Signal-Regulated Kinases, and Nuclear Factor Kappa B Signaling Pathways
by Zerrin Barut, Mutay Aslan, Bürke Çırçırlı, Tuğçe Çeker and Çağatay Yılmaz
Pharmaceuticals 2024, 17(7), 860; https://doi.org/10.3390/ph17070860 - 1 Jul 2024
Cited by 1 | Viewed by 1535
Abstract
Background: This study aimed to examine the effect of 7-Ketositosterol (7-KSS), on sphingomyelin/ceramide metabolites and apoptosis in human breast MCF-7 and human liver HepG2 cancer cells. Methods: Anti-proliferative effects of 7-KSS treatment were assessed at different concentrations and periods. Cell viability [...] Read more.
Background: This study aimed to examine the effect of 7-Ketositosterol (7-KSS), on sphingomyelin/ceramide metabolites and apoptosis in human breast MCF-7 and human liver HepG2 cancer cells. Methods: Anti-proliferative effects of 7-KSS treatment were assessed at different concentrations and periods. Cell viability was assessed through MTT analysis, whereas the levels of sphingosine-1-phosphate (S1P), sphingomyelins (SMs), and ceramides (CERs) were measured using LC-MS/MS. Phosphorylated 44/42 ERK1/2 and NF-κB p65 (Ser536) protein levels were measured by Western blot analysis and immunofluorescence staining. Apoptosis was evaluated by TUNEL staining and flow cytometric assessment of annexin-V and propidium iodide (PI) labeling. Results: Treatment with 7-KSS significantly decreased cell survival and S1P, p-44/42 ERK1/2, and p-NF-κB p65 protein levels in cancer cells compared to controls. A substantial rise was detected in intracellular amounts of C16-C24 CERs and apoptosis in cancer cells incubated with 7-KSS. Conclusions: 7-KSS stimulated ceramide accumulation and apoptosis while decreasing cell proliferation via downregulating S1P, p-44/42 ERK1/2, and p-NF-κB p65 protein levels. Full article
(This article belongs to the Special Issue Novel Anti-proliferative Agents, 2nd Edition)
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18 pages, 1712 KiB  
Article
Synthesis and Study of the Structure–Activity Relationship of Antiproliferative N-Substituted Isosteviol-Based 1,3-Aminoalcohols
by Dániel Ozsvár, Noémi Bózsity, István Zupkó and Zsolt Szakonyi
Pharmaceuticals 2024, 17(2), 262; https://doi.org/10.3390/ph17020262 - 19 Feb 2024
Cited by 2 | Viewed by 1430
Abstract
Starting from isosteviol, a series of diterpenoid 1,3-aminoalcohol derivatives were prepared via stereoselective transformations. The acid-catalysed hydrolysis and rearrangement of natural stevioside produced isosteviol, which was transformed into the key intermediate methyl ester. In the next step, an 1,3-aminoalcohol library was prepared by [...] Read more.
Starting from isosteviol, a series of diterpenoid 1,3-aminoalcohol derivatives were prepared via stereoselective transformations. The acid-catalysed hydrolysis and rearrangement of natural stevioside produced isosteviol, which was transformed into the key intermediate methyl ester. In the next step, an 1,3-aminoalcohol library was prepared by the reductive amination of the intermediate 3-hydroxyaldehyde obtained from isosteviol in a two-step synthesis. To study the effect of the carboxylate ester function at position 4, the free carboxylic acid, benzyl ester and acryloyl ester analogues were prepared as elongated derivatives in comparison with our earlier results in this field. The antiproliferative activity of compounds against human tumour cell lines (A2780, HeLa, MCF-7 and MDA-MB-231) was investigated. In our preliminary study, the 1,3-aminoalcohol function with N-benzyl or (1H-imidazol-1-yl)-propyl substitution and benzyl ester moiety seemed essential for the reliable antiproliferative activity. The results obtained could be a good starting point to further functionalisation towards more efficient antiproliferative diterpenes. Full article
(This article belongs to the Special Issue Novel Anti-proliferative Agents, 2nd Edition)
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13 pages, 4197 KiB  
Communication
Design, Synthesis, In Vitro, and In Silico Studies of New N5-Substituted-pyrazolo[3,4-d]pyrimidinone Derivatives as Anticancer CDK2 Inhibitors
by Waheed A. Zaki, Selwan M. El-Sayed, Mohamed Alswah, Ahmed El-Morsy, Ashraf H. Bayoumi, Abrahman S. Mayhoub, Walaa H. Moustafa, Aeshah A. Awaji, Eun Joo Roh, Ahmed H.E. Hassan and Kazem Mahmoud
Pharmaceuticals 2023, 16(11), 1593; https://doi.org/10.3390/ph16111593 - 11 Nov 2023
Cited by 3 | Viewed by 2026
Abstract
CDK2 is a key player in cell cycle processes. It has a crucial role in the progression of various cancers. Hepatocellular carcinoma (HCC) and colorectal cancer (CRC) are two common cancers that affect humans worldwide. The available therapeutic options suffer from many drawbacks [...] Read more.
CDK2 is a key player in cell cycle processes. It has a crucial role in the progression of various cancers. Hepatocellular carcinoma (HCC) and colorectal cancer (CRC) are two common cancers that affect humans worldwide. The available therapeutic options suffer from many drawbacks including high toxicity and decreased specificity. Therefore, there is a need for more effective and safer therapeutic agents. A series of new pyrazolo[3,4-d]pyrimidine analogs was designed, synthesized, and evaluated as anticancer agents against the CRC and HCC cells, HCT116, and HepG2, respectively. Pyrazolo[3,4-d]pyrimidinone derivatives bearing N5-2-(4-halophenyl) acetamide substituents were identified as the most potent amongst evaluated compounds. Further evaluation of CDK2 kinase inhibition of two potential cytotoxic compounds 4a and 4b confirmed their CDK2 inhibitory activity. Compound 4a was more potent than the reference roscovitine regarding the CDK2 inhibitory activity (IC50 values: 0.21 and 0.25 µM, respectively). In silico molecular docking provided insights into the molecular interactions of compounds 4a and 4b with important amino acids within the ATP-binding site of CDK2 (Ile10, Leu83, and Leu134). Overall, compounds 4a and 4b were identified as interesting CDK2 inhibitors eliciting antiproliferative activity against the CRC and HCC cells, HCT116 and HepG2, respectively, for future further investigations and development. Full article
(This article belongs to the Special Issue Novel Anti-proliferative Agents, 2nd Edition)
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Review

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36 pages, 7093 KiB  
Review
The Therapeutic Potential of Spirooxindoles in Cancer: A Focus on p53–MDM2 Modulation
by Adel S. Girgis, Yujun Zhao, Angel Nkosi, Nasser S. M. Ismail, Mohamed S. Bekheit, Dalia R. Aboshouk, Marian N. Aziz, M. Adel Youssef and Siva S. Panda
Pharmaceuticals 2025, 18(2), 274; https://doi.org/10.3390/ph18020274 - 19 Feb 2025
Viewed by 815
Abstract
The p53, often referred to as the “guardian of the genome”, is a well-established tumor-suppressor protein that plays a critical role in regulating the cell cycle, DNA repair, differentiation, and apoptosis, with its activity primarily modulated by the MDM2 protein (murine double minute [...] Read more.
The p53, often referred to as the “guardian of the genome”, is a well-established tumor-suppressor protein that plays a critical role in regulating the cell cycle, DNA repair, differentiation, and apoptosis, with its activity primarily modulated by the MDM2 protein (murine double minute 2, also known as HDM2 in humans). Disrupting the protein-protein interaction between p53 and MDM2 represents a promising therapeutic strategy for developing anticancer agents. Recent studies have shown that several spirooxindole-containing compounds exhibit significant antitumor properties, primarily by inhibiting the p53–MDM2 interaction. This review provides an overview of structure-based spirooxindoles that could have therapeutic potential. It highlights findings from the past decade concerning their antiproliferative properties and implications for interfering with the p53–MDM2 interaction. The discussion includes various analogs of spirooxindoles as promising candidates for optimizing leads in drug discovery programs aimed at developing novel and clinically effective agents. Full article
(This article belongs to the Special Issue Novel Anti-proliferative Agents, 2nd Edition)
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23 pages, 3865 KiB  
Review
From Infection to Tumor: Exploring the Therapeutic Potential of Ciprofloxacin Derivatives as Anticancer Agents
by Hesham M. Hassan, Roket Hassan, Ranya Mohammed Elmagzoub, Ahmed Al-Emam, Konstantinos Kossenas, Ahmed S. Abdel-Samea, Hazim O. Khalifa, Suleyman Akocak, Stefan Bräse and Hamada Hashem
Pharmaceuticals 2025, 18(1), 72; https://doi.org/10.3390/ph18010072 - 9 Jan 2025
Viewed by 1622
Abstract
Ciprofloxacin, a widely used second-generation fluoroquinolone for treating bacterial infections, has recently shown notable anticancer properties. This review explores progress in developing ciprofloxacin derivatives with anticancer properties, emphasizing key structural changes that improve their therapeutic effectiveness by modifying the basic group at position [...] Read more.
Ciprofloxacin, a widely used second-generation fluoroquinolone for treating bacterial infections, has recently shown notable anticancer properties. This review explores progress in developing ciprofloxacin derivatives with anticancer properties, emphasizing key structural changes that improve their therapeutic effectiveness by modifying the basic group at position 7, the carboxylic acid group at position 3, or both. It further investigates the mechanisms by which these derivatives fight cancer, such as inducing apoptosis, arresting the cell cycle, inhibiting topoisomerase I and II, preventing tubulin polymerization, suppressing interleukin 6, blocking thymidine phosphorylase, inhibiting multidrug resistance proteins, and hindering angiogenesis. Additionally, it outlines their future directions, such as enhancing their efficacy, selectivity, and investigating potential synergy with other chemotherapeutic agents, offering a promising avenue for developing new therapies for cancer. Full article
(This article belongs to the Special Issue Novel Anti-proliferative Agents, 2nd Edition)
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