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Bioactive Compounds in Cancers
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Bioactive Compounds in Cancers

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

Deadline for manuscript submissions: 20 July 2024 | Viewed by 3028

Special Issue Editors

Dr. Patricia M. A. Silva

E-Mail Website
Guest Editor
1. UNIPRO – Oral Pathology and Rehabilitation Research Unit, University Institute of Health Sciences (IUCS-CESPU), 4585-116 Gandra, Portugal
2. TOXRUN – Toxicology Research Unit, University Institute of Health Sciences, CESPU, CRL, 4585-116 Gandra, Portugal
Interests: anticancer strategies; targeted therapy; mitosis; apoptosis; drug screening; bioactive compounds
Special Issues, Collections and Topics in MDPI journals
Dr. Honorina Cidade

E-Mail Website
Guest Editor
Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira n° 228, 4050-313 Porto, Portugal
Interests: medicinal chemistry; organic synthesis; drug discovery; anticancer activity; antimicrobial activity; chiral drugs; natural products
Special Issues, Collections and Topics in MDPI journals
Dr. Hassan Bousbaa

E-Mail Website
Guest Editor
UNIPRO – Unidade de Investigação em Patologia e Reabilitação Oral, IUCS, CESPU, Rua Central de Gandra, 1317, 4585-116 Gandra PRD, Portugal
Interests: targeted anticancer therapy; targeting mitosis for cancer therapy; antimitotic agents; biological evaluation of natural and synthetic compounds; cancer biomarkers
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Cancer is one of the leading causes of death worldwide, and its incidence continues to increase dramatically. The estimated number of new cases from 2020 to 2040 is 10.9 million (a 56.5% increase), and thus this topic continues to be relevant. The complexity of cancer identities, the individuality of each patient, and the emergence of resistance to cancer treatment make it difficult to obtain the desired clinical benefit, largely contributing to the large numbers. In the cancer research field, several therapeutic strategies have been extensively explored, from the discovery of new bioactive compounds to the repurposing of currently available drugs, yet challenges remain. In this regard, and given the chemistry diversity in nature, the use of compounds based on natural sources, including plants, bacteria, or other living organisms, has gained particular attention as they could be more reliable, economical, and safer.

Hence, this research topic aims to highlight the recent advances and breakthroughs in emerging anticancer strategies based on bioactive compounds alone or in combination with other clinical standard treatments, providing scientific evidence on their mechanisms of action.

We welcome submissions of original research and review articles. Topics for this Special Issue include, but are not limited to:

  • Identification of novel bioactive compounds with anticancer potential;
  • Characterization/Elucidation of the mechanism of action of new or old bioactive compounds;
  • Methodologies and models to study and characterize bioactive compounds in cancers;
  • Strategies of drug delivery for bioactive compounds in cancers.

Dr. Patricia M. A. Silva
Dr. Honorina Cidade
Dr. Hassan Bousbaa
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at mdpi.longhoe.net 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 strategies
  • bioactive compounds
  • natural products
  • synthetic products
  • medicinal chemistry
  • drug repurposing
  • drug delivery systems

Published Papers (3 papers)

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Research

22 pages, 3850 KiB  
Article
Synthesis, Anticancer Activity, and Docking Studies of Novel Hydroquinone-Chalcone-Pyrazoline Hybrid Derivatives
by Javier Maldonado, Alfonso Oliva, Leda Guzmán, Aurora Molinari and Waldo Acevedo
Int. J. Mol. Sci. 2024, 25(13), 7281; https://doi.org/10.3390/ijms25137281 - 2 Jul 2024
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Abstract
A novel series of antitumor hybrids was synthesized using 1,4-benzohydroquinone and chalcone, furane, or pyrazoline scaffolds. This were achieved through isosteric substitution of the aryl group of the chalcone β-carbon with the furanyl moiety and structural modification of the α,β-unsaturated carbonyl system. The [...] Read more.
A novel series of antitumor hybrids was synthesized using 1,4-benzohydroquinone and chalcone, furane, or pyrazoline scaffolds. This were achieved through isosteric substitution of the aryl group of the chalcone β-carbon with the furanyl moiety and structural modification of the α,β-unsaturated carbonyl system. The potential antitumor activity of these hybrids was evaluated in vivo on MCF-7 breast adenocarcinoma and HT-29 colorectal carcinoma cells, demonstrating cytotoxic activity with IC50 values ranging from 28.8 to 124.6 µM. The incorporation of furan and pyrazoline groups significantly enhanced antiproliferative properties compared to their analogues and precursors (VII–X), which were inactive against both neoplastic cell lines. Compounds 4, 5, and 6 exhibited enhanced cytotoxicity against both cell lines, whereas compound 8 showed higher cytotoxic activity against HT-29 cells. Molecular docking studies revealed superior free-energy values (ΔGbin) for carcinogenic pathway-involved kinase proteins, with our in silico data suggesting that these derivatives could be promising chemotherapeutic agents targeting kinase pathways. Among all the synthesized PIBHQ compounds, derivatives 7 and 8 exhibited the best drug-likeness properties, with values of 0.53 and 0.83, respectively. ADME results collectively suggest that most of these compounds hold promise as potential candidates for preclinical assays. Full article
(This article belongs to the Special Issue Bioactive Compounds in Cancers)
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19 pages, 6375 KiB  
Article
Evaluation of Antitumor Activity of Xanthones Conjugated with Amino Acids
by Flávia Barbosa, Joana Araújo, Virgínia M. F. Gonçalves, Andreia Palmeira, Andrea Cunha, Patrícia M. A. Silva, Carla Fernandes, Madalena Pinto, Hassan Bousbaa, Odília Queirós and Maria Elizabeth Tiritan
Int. J. Mol. Sci. 2024, 25(4), 2121; https://doi.org/10.3390/ijms25042121 - 9 Feb 2024
Viewed by 1021
Abstract
Cancer is a complex disease characterized by several alterations, which confer, to the cells, the capacity to proliferate uncontrollably and to resist cellular death. Multiresistance to conventional chemotherapy drugs is often the cause of treatment failure; thus, the search for natural products or [...] Read more.
Cancer is a complex disease characterized by several alterations, which confer, to the cells, the capacity to proliferate uncontrollably and to resist cellular death. Multiresistance to conventional chemotherapy drugs is often the cause of treatment failure; thus, the search for natural products or their derivatives with therapeutic action is essential. Chiral derivatives of xanthones (CDXs) have shown potential inhibitory activity against the growth of some human tumor cell lines. This work reports the screening of a library of CDXs, through viability assays, in different cancer cell lines: A375-C5, MCF-7, NCI-H460, and HCT-15. CDXs’ effect was analyzed based on several parameters of cancer cells, and it was also verified if these compounds were substrates of glycoprotein-P (Pgp), one of the main mechanisms of resistance in cancer therapy. Pgp expression was evaluated in all cell lines, but no expression was observed, except for HCT-15. Also, when a humanized yeast expressing the human gene MDR1 was used, no conclusions could be drawn about CDXs as Pgp substrates. The selected CDXs did not induce significant differences in the metabolic parameters analyzed. These results show that some CDXs present promising antitumor activity, but other mechanisms should be triggered by these compounds. Full article
(This article belongs to the Special Issue Bioactive Compounds in Cancers)
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20 pages, 5517 KiB  
Article
BP-M345 as a Basis for the Discovery of New Diarylpentanoids with Promising Antimitotic Activity
by Joana Moreira, Patrícia M. A. Silva, Eliseba Castro, Lucília Saraiva, Madalena Pinto, Hassan Bousbaa and Honorina Cidade
Int. J. Mol. Sci. 2024, 25(3), 1691; https://doi.org/10.3390/ijms25031691 - 30 Jan 2024
Cited by 1 | Viewed by 849
Abstract
Recently, the diarylpentanoid BP-M345 (5) has been identified as a potent in vitro growth inhibitor of cancer cells, with a GI50 value between 0.17 and 0.45 µM, showing low toxicity in non-tumor cells. BP-M345 (5) promotes mitotic arrest [...] Read more.
Recently, the diarylpentanoid BP-M345 (5) has been identified as a potent in vitro growth inhibitor of cancer cells, with a GI50 value between 0.17 and 0.45 µM, showing low toxicity in non-tumor cells. BP-M345 (5) promotes mitotic arrest by interfering with mitotic spindle assembly, leading to apoptotic cell death. Following on from our previous work, we designed and synthesized a library of BP-M345 (5) analogs and evaluated the cell growth inhibitory activity of three human cancer cell lines within this library in order to perform structure–activity relationship (SAR) studies and to obtain compounds with improved antimitotic effects. Four compounds (7, 9, 13, and 16) were active, and the growth inhibition effects of compounds 7, 13, and 16 were associated with a pronounced arrest in mitosis. These compounds exhibited a similar or even higher mitotic index than BP-M345 (5), with compound 13 displaying the highest antimitotic activity, associated with the interference with mitotic spindle dynamics, inducing spindle collapse and, consequently, prolonged mitotic arrest, culminating in massive cancer cell death by apoptosis. Full article
(This article belongs to the Special Issue Bioactive Compounds in Cancers)
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