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Translational Approach to Antitumor Drugs - 2nd Edition
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Translational Approach to Antitumor Drugs - 2nd Edition

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (28 February 2022) | Viewed by 22301

Special Issue Editors

Prof. Dr. Krešimir Pavelić

E-Mail Website
Guest Editor
Faculty of Medicine, Juraj Dobrila University of Pula, Pula, Croatia
Interests: oncology; tumor genetic; molecular medicine; personalized medicine; drug development; zeolite; medical devices
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Sandra Kraljević Pavelić

E-Mail Website
Guest Editor
Faculty of Health Studies, University of Rijeka, Rijeka, Croatia
Interests: drug development; study of biomarkers; clinoptilolite research; high-throughput analytics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In recent decades, a significant step was achieved when malignancies started to be managed as chronic diseases. However, cancer remains a big problem and there is a huge need for new effective drugs and treatments. As a continuation to the previous Special Issue, we will cover a wide range of drug development topics, including research of molecular biomarkers, pattern identification, and pro-drugs design. Development of new drugs and treatments involves a broad translational approach to research that includes various topics, i.e., treatment methods and types, new small molecules, newly synthesized organic compounds, synthetic or purified natural products originating from the sea or on land, medical devices and inorganic compounds, and novel biomarkers. In this issue, we will put the focus on the translational potential of data generated within the drug development process. This issue therefore aims to provide an extended forum for dissemination of the latest information on some new potential anticancer drugs, treatments or drug targets, and methods for testing of their potential. Clinical trial data is accordingly appropriate for submission as well.

Prof. Dr. Krešimir Pavelić
Prof. Dr. Sandra Kraljević Pavelić
Guest Editors

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Keywords

  • natural compounds or derivatives in cancer treatment
  • synthesis, computational analysis of novel organic compounds
  • inorganic compounds in cancer treatment
  • management of cancer therapy-induced side effects
  • cancer biomarker analyses including proteome, secretome and N-glycome profiling of chemoresistant cancer cells
  • immunohistochemistry or molecular profiles in cancer patients
  • clinical trials of new cancer therapies

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Published Papers (5 papers)

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Research

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18 pages, 5200 KiB  
Article
Synthesis and Antimicrobial, Anticancer and Anti-Oxidant Activities of Novel 2,3-Dihydropyrido[2,3-d]pyrimidine-4-one and Pyrrolo[2,1-b][1,3]benzothiazole Derivatives via Microwave-Assisted Synthesis
by Aamal A. Al-Mutairi, Hend N. Hafez, Abdel-Rhaman B. A. El-Gazzar and Marwa Y. A. Mohamed
Molecules 2022, 27(4), 1246; https://doi.org/10.3390/molecules27041246 - 12 Feb 2022
Cited by 8 | Viewed by 2826
Abstract
In our attempt towards the synthesis and development of effective antimicrobial, anticancer and antioxidant agents, a novel series of 2,3-dihydropyrido[2,3-d]pyrimidin-4-one 7a–e and pyrrolo[2,1-b][1,3]benzothiazoles 9a–e were synthesized. The synthesis of 2-(1,3-benzo thiazol-2-yl)-3-(aryl)prop-2-enenitrile (5a–e) as the key [...] Read more.
In our attempt towards the synthesis and development of effective antimicrobial, anticancer and antioxidant agents, a novel series of 2,3-dihydropyrido[2,3-d]pyrimidin-4-one 7a–e and pyrrolo[2,1-b][1,3]benzothiazoles 9a–e were synthesized. The synthesis of 2-(1,3-benzo thiazol-2-yl)-3-(aryl)prop-2-enenitrile (5a–e) as the key intermediate was accomplished by a microwave efficient method. Via a new variety oriented synthetic microwave pathway, these highly functionalized building blocks allowed access to numerous fused heteroaromatic such as 7-amino-6-(1,3-benzo thiazol-2-yl)-5-(aryl)-2-thioxo-2,3dihydropyrido [2,3-d]pyrimidin-4(1H)-one 7a–e and 1-amino-2-(aryl)pyrrolo[2,1-b][1,3]benzothiazole-3-carbonitrile derivatives 9a–e in order to study their antimicrobial and anticancer activity. The present investigation offers effective and rapid new procedures for the synthesis of the newly polycondensed heterocyclic ring systems. All the newly synthesized compounds were evaluated for antimicrobial, anticancer and antioxidant activity. Compounds 7a,d, and 9a,d showed higher antimicrobial activity than cefotaxime and fluconazole while the remaining compounds exhibited good to moderate activity against bacteria and fungi. An anticancer evaluation of the newly synthesized compounds against the three tumor cell lines (lung cell NCI-H460, liver cancer HepG2 and colon cancer HCT-116) exhibited that compounds 7a, d, and 9a,d have higher cytotoxicity against the three human cell lines compared to doxorubicin as a reference drug. These compounds also exhibited higher antioxidant activity and a great ability to protect DNA from damage induced by bleomycin. Full article
(This article belongs to the Special Issue Translational Approach to Antitumor Drugs - 2nd Edition)
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21 pages, 27284 KiB  
Article
Chemical Evaluation, Antioxidant, Antiproliferative, Anti-Inflammatory and Antibacterial Activities of Organic Extract and Semi-Purified Fractions of the Adriatic Sea Fan, Eunicella cavolini
by Dario Matulja, Petra Grbčić, Krunoslav Bojanić, Natalija Topić-Popović, Rozelindra Čož-Rakovac, Sylvain Laclef, Tomislav Šmuc, Ozren Jović, Dean Marković and Sandra Kraljević Pavelić
Molecules 2021, 26(19), 5751; https://doi.org/10.3390/molecules26195751 - 23 Sep 2021
Cited by 5 | Viewed by 3704
Abstract
Due to sedentary lifestyle and harsh environmental conditions, gorgonian coral extracts are recognized as a rich source of novel compounds with various biological activities, of interest to the pharmaceutical and cosmetic industries. The presented study aimed to perform chemical screening of organic extracts [...] Read more.
Due to sedentary lifestyle and harsh environmental conditions, gorgonian coral extracts are recognized as a rich source of novel compounds with various biological activities, of interest to the pharmaceutical and cosmetic industries. The presented study aimed to perform chemical screening of organic extracts and semi-purified fractions obtained from the common Adriatic gorgonian, sea fan, Eunicella cavolini (Koch, 1887) and explore its abilities to exert different biological effects in vitro. Qualitative chemical evaluation revealed the presence of several classes of secondary metabolites extended with mass spectrometry analysis and tentative dereplication by using Global Natural Product Social Molecular Networking online platform (GNPS). Furthermore, fractions F4 and F3 showed the highest phenolic (3.28 ± 0.04 mg GAE/g sample) and carotene (23.11 ± 2.48 mg β-CA/g sample) content, respectively. The fraction F3 inhibited 50% of DPPH (2,2-diphenyl-1-picryl-hydrazyl-hydrate) and ABTS (2,2′-azino-bis (3-ethylbenzthiazolin-6-yl) sulfonic acid) radicals at the concentrations of 767.09 ± 11.57 and 157.16 ± 10.83 µg/mL, respectively. The highest anti-inflammatory potential was exhibited by F2 (IC50 = 198.70 ± 28.77 µg/mL) regarding the inhibition of albumin denaturation and F1 (IC50 = 254.49 ± 49.17 µg/mL) in terms of soybean lipoxygenase inhibition. In addition, the most pronounced antiproliferative effects were observed for all samples (IC50 ranging from 0.82 ± 0.14–231.18 ± 46.13 µg/mL) against several carcinoma cell lines, but also towards non-transformed human fibroblasts pointing to a generally cytotoxic effect. In addition, the antibacterial activity was tested by broth microdilution assay against three human pathogenic bacteria: Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus. The latter was the most affected by fractions F2 and F3. Finally, further purification, isolation and characterization of pure compounds from the most active fractions are under investigation. Full article
(This article belongs to the Special Issue Translational Approach to Antitumor Drugs - 2nd Edition)
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26 pages, 4085 KiB  
Article
Novel Bis- and Mono-Pyrrolo[2,3-d]pyrimidine and Purine Derivatives: Synthesis, Computational Analysis and Antiproliferative Evaluation
by Andrea Bistrović Popov, Robert Vianelo, Petra Grbčić, Mirela Sedić, Sandra Kraljević Pavelić, Krešimir Pavelić and Silvana Raić-Malić
Molecules 2021, 26(11), 3334; https://doi.org/10.3390/molecules26113334 - 1 Jun 2021
Cited by 7 | Viewed by 3434
Abstract
Novel symmetrical bis-pyrrolo[2,3-d]pyrimidines and bis-purines and their monomers were synthesized and evaluated for their antiproliferative activity in human lung adenocarcinoma (A549), cervical carcinoma (HeLa), ductal pancreatic adenocarcinoma (CFPAC-1) and metastatic colorectal adenocarcinoma (SW620) cells. The use of ultrasound irradiation as alternative [...] Read more.
Novel symmetrical bis-pyrrolo[2,3-d]pyrimidines and bis-purines and their monomers were synthesized and evaluated for their antiproliferative activity in human lung adenocarcinoma (A549), cervical carcinoma (HeLa), ductal pancreatic adenocarcinoma (CFPAC-1) and metastatic colorectal adenocarcinoma (SW620) cells. The use of ultrasound irradiation as alternative energy input in Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) shortened the reaction time, increased the reaction efficiency and led to the formation of exclusively symmetric bis-heterocycles. DFT calculations showed that triazole formation is exceedingly exergonic and confirmed that the presence of Cu(I) ions is required to overcome high kinetic requirements and allow the reaction to proceed. The influence of various linkers and 6-substituted purine and regioisomeric 7-deazapurine on their cytostatic activity was revealed. Among all the evaluated compounds, the 4-chloropyrrolo[2,3-d]pyrimidine monomer 5f with 4,4′-bis(oxymethylene)biphenyl had the most pronounced, although not selective, growth-inhibitory effect on pancreatic adenocarcinoma (CFPAC-1) cells (IC50 = 0.79 µM). Annexin V assay results revealed that its strong growth inhibitory activity against CFPAC-1 cells could be associated with induction of apoptosis and primary necrosis. Further structural optimization of bis-chloropyrrolo[2,3-d]pyrimidine with aromatic linker is required to develop novel efficient and non-toxic agent against pancreatic cancer. Full article
(This article belongs to the Special Issue Translational Approach to Antitumor Drugs - 2nd Edition)
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Review

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45 pages, 2669 KiB  
Review
Proteomic Research on the Antitumor Properties of Medicinal Mushrooms
by Boris Jakopovic, Nada Oršolić and Ivan Jakopovich
Molecules 2021, 26(21), 6708; https://doi.org/10.3390/molecules26216708 - 5 Nov 2021
Cited by 16 | Viewed by 4729
Abstract
Medicinal mushrooms are increasingly being recognized as an important therapeutic modality in complementary oncology. Until now, more than 800 mushroom species have been known to possess significant pharmacological properties, of which antitumor and immunomodulatory properties have been the most researched. Besides a number [...] Read more.
Medicinal mushrooms are increasingly being recognized as an important therapeutic modality in complementary oncology. Until now, more than 800 mushroom species have been known to possess significant pharmacological properties, of which antitumor and immunomodulatory properties have been the most researched. Besides a number of medicinal mushroom preparations being used as dietary supplements and nutraceuticals, several isolates from mushrooms have been used as official antitumor drugs in clinical settings for several decades. Various proteomic approaches allow for the identification of a large number of differentially regulated proteins serendipitously, thereby providing an important platform for a discovery of new potential therapeutic targets and approaches as well as biomarkers of malignant disease. This review is focused on the current state of proteomic research into antitumor mechanisms of some of the most researched medicinal mushroom species, including Phellinus linteus, Ganoderma lucidum, Auricularia auricula, Agrocybe aegerita, Grifola frondosa, and Lentinus edodes, as whole body extracts or various isolates, as well as of complex extract mixtures. Full article
(This article belongs to the Special Issue Translational Approach to Antitumor Drugs - 2nd Edition)
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33 pages, 740 KiB  
Review
Effects of Zeolite as a Drug Delivery System on Cancer Therapy: A Systematic Review
by Jessica Hao, Ivana Stavljenić Milašin, Zeynep Batu Eken, Marinka Mravak-Stipetic, Krešimir Pavelić and Fusun Ozer
Molecules 2021, 26(20), 6196; https://doi.org/10.3390/molecules26206196 - 14 Oct 2021
Cited by 35 | Viewed by 6483
Abstract
Zeolites and zeolitic imidazolate frameworks (ZIFs) are widely studied as drug carrying nanoplatforms to enhance the specificity and efficacy of traditional anticancer drugs. At present, there is no other systematic review that assesses the potency of zeolites/ZIFs as anticancer drug carriers. Due to [...] Read more.
Zeolites and zeolitic imidazolate frameworks (ZIFs) are widely studied as drug carrying nanoplatforms to enhance the specificity and efficacy of traditional anticancer drugs. At present, there is no other systematic review that assesses the potency of zeolites/ZIFs as anticancer drug carriers. Due to the porous nature and inherent pH-sensitive properties of zeolites/ZIFs, the compounds can entrap and selectively release anticancer drugs into the acidic tumor microenvironment. Therefore, it is valuable to provide a comprehensive overview of available evidence on the topic to identify the benefits of the compound as well as potential gaps in knowledge. The purpose of this study was to evaluate the potential therapeutic applications of zeolites/ZIFs as drug delivery systems delivering doxorubicin (DOX), 5-fluorouracil (5-FU), curcumin, cisplatin, and miR-34a. Following PRISMA guidelines, an exhaustive search of PubMed, Scopus, Embase, and Web of Science was conducted. No language or time limitations were used up to 25th August 2021. Only full text articles were selected that pertained to the usage of zeolites/ZIFs in delivering anticancer drugs. Initially, 1279 studies were identified, of which 572 duplicate records were excluded. After screening for the title, abstract, and full texts, 53 articles remained and were included in the qualitative synthesis. An Inter-Rater Reliability (IRR) test, which included a percent user agreement and reliability percent, was conducted for the 53 articles. The included studies suggest that anticancer drug-incorporated zeolites/ZIFs can be used as alternative treatment options to enhance the efficacy of cancer treatment by mitigating the drawbacks of drugs under conventional treatment. Full article
(This article belongs to the Special Issue Translational Approach to Antitumor Drugs - 2nd Edition)
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