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Special Issue "Recent Advances in Anticancer Drugs"

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

Deadline for manuscript submissions: 28 February 2019

Special Issue Editors

Guest Editor
Prof. Dr. Simona Collina

Centre for Health Technologies (CHT), Department of Drug Sciences, Medicinal Chemistry and
Pharmaceutical Technology Section, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy
Website | E-Mail
Interests: rational drug design, synthesis and structure-activity relationships of biologically active compounds (small molecules and peptides); preparation and characterization of chiral compounds, discovery of new modulators of sigma receptors as well as of small molecules able to affect the protein kinase C (PKC)/ELAV proteins/mRNA system
Guest Editor
Prof. Dr. Mariarosaria Miloso

School of Medicine and Surgery, University of Milano-Bicocca, Via Cadore 48, 20900 Monza, Italy
Website | E-Mail
Interests: evaluation of antitumorigenic effects of natural and synthetic compounds; characterization of biological properties of mesenchymal stem cells from different sources

Special Issue Information

Dear Colleagues,

Cancer is the second leading cause of death, being responsible for almost one in six deaths globally. The World Health Organization (WHO) highlights that cancer no longer needs to be a death sentence, as the capacity exists to reduce its burden and improve the survival and quality of life of people living with the disease. Technological and scientific advances facilitate the study of tumour biology and the identification of novel therapeutic targets, allowing the transition from cytotoxic chemotherapy to targeted cancer therapies. Compounds targeting specific cellular processes have been designed and biomarkers useful for the early diagnosis and for the transition of new molecules from the preclinical to the clinical stage identified. Nevertheless, oncology drug discovery and development remain a challenge for all the scientists working in this field.

This Special Issue of Molecules will cover the major advancements and challenges of cancer drug discovery. It will report on the identification and evaluation of novel anticancer agents, biological targets and therapeutic approaches, original researches and review articles on exploring antitumor drugs.

We cordially invite researchers working in this field to contribute original research articles, short communications, and critical review articles. Short papers on one compound will be also welcome.

Prof. Dr. Simona Collina
Prof. Dr. Mariarosaria Miloso
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 papers will be 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. Molecules 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 1800 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

  • Anticancer drugs
  • Drug discovery
  • Biological targets
  • Therapeutic approaches
  • Biomarkers

Published Papers (3 papers)

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Research

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Open AccessArticle Somatostatin Receptors as Molecular Targets in Human Uveal Melanoma
Molecules 2018, 23(7), 1535; https://doi.org/10.3390/molecules23071535
Received: 29 May 2018 / Revised: 20 June 2018 / Accepted: 22 June 2018 / Published: 26 June 2018
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Abstract
Uveal melanoma (UM) is the most common primary intraocular malignancy in adults, with an incidence of 4–5 cases per million. The prognosis of UM is very poor. In the present study, our aim was to investigate the expression of mRNA and protein for
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Uveal melanoma (UM) is the most common primary intraocular malignancy in adults, with an incidence of 4–5 cases per million. The prognosis of UM is very poor. In the present study, our aim was to investigate the expression of mRNA and protein for somatostatin receptor types-1, -2, -3, -4, -5 (SSTR-1–5) in human UM tissue samples and in OCM-1 and OCM-3 human UM cell lines by qRT-PCR, western blot and ligand competition assay. The mRNA for SSTR-2 showed markedly higher expression in UM tissues than SSTR-5. The presence of SSTRs was demonstrated in 70% of UM specimens using ligand competition assay and both human UM models displayed specific high affinity SSTRs. Among the five SSTRs, the mRNA investigated for SSTR-2 and SSTR-5 receptors was strongly expressed in both human UM cell lines, SSTR-5 showing the highest expression. The presence of the SSTR-2 and SSTR-5 receptor proteins was confirmed in both cell lines by western blot. In summary, the expression of somatostatin receptors in human UM specimens and in OCM-1 and OCM-3 human UM cell lines suggests that they could serve as a potential molecular target for therapy of UM using modern powerful cytotoxic SST analogs targeting SSTR-2 and SSTR-5 receptors. Full article
(This article belongs to the Special Issue Recent Advances in Anticancer Drugs)
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Open AccessArticle Pyridine-Ureas as Potential Anticancer Agents: Synthesis and In Vitro Biological Evaluation
Molecules 2018, 23(6), 1459; https://doi.org/10.3390/molecules23061459
Received: 23 May 2018 / Revised: 12 June 2018 / Accepted: 12 June 2018 / Published: 15 June 2018
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Abstract
In our endeavor towards the development of effective anticancer agents, a novel series of pyridine-ureas 8an were synthesized. All the newly prepared derivatives were evaluated in vitro for their growth inhibitory activity towards the proliferation of breast cancer MCF-7 cell line.
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In our endeavor towards the development of effective anticancer agents, a novel series of pyridine-ureas 8an were synthesized. All the newly prepared derivatives were evaluated in vitro for their growth inhibitory activity towards the proliferation of breast cancer MCF-7 cell line. Compounds 8e and 8n were found to be the most active congeners against MCF-7 cells (IC50 = 0.22 and 1.88 µM after 48 h treatment; 0.11 and 0.80 µM after 72 h treatment, respectively) with increased activity compared to the reference drug doxorubicin (IC50 = 1.93 µM). Moreover, eight selected pyridines 8b, 8d, 8e, 8i, 8j and 8ln were evaluated for their in vitro anticancer activity according to the US-NCI protocol. Pyridines 8b and 8e proved to be the most effective anticancer agents in the NCI assay with mean inhibition = 43 and 49%, respectively. Both 8b and 8e exhibited anti-proliferative activity against all tested cancer cell lines from all subpanels growth inhibition (GI for 8b; 12–78%, GI for 8e; 15–91%). Pyridines 8b and 8e were screened in vitro for their inhibitory activity against VEGFR-2. Both compounds inhibited VEGFR-2 at micromolar IC50 values 5.0 ± 1.91 and 3.93 ± 0.73 µM, respectively. The most active pyridines were filtered according to the Lipinski and Veber rules and all of them passed these filters. Finally, several ADME descriptors were predicted for the active pyridines through a theoretical kinetic study. Full article
(This article belongs to the Special Issue Recent Advances in Anticancer Drugs)
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Review

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Open AccessReview Mitochondria-Targeting Small Molecules Effectively Prevent Cardiotoxicity Induced by Doxorubicin
Molecules 2018, 23(6), 1486; https://doi.org/10.3390/molecules23061486
Received: 22 May 2018 / Revised: 13 June 2018 / Accepted: 13 June 2018 / Published: 19 June 2018
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Abstract
Doxorubicin (Dox) is a chemotherapeutic agent widely used for the treatment of numerous cancers. However, the clinical use of Dox is limited by its unwanted cardiotoxicity. Mitochondrial dysfunction has been associated with Dox-induced cardiotoxicity. To mitigate Dox-related cardiotoxicity, considerable successful examples of a
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Doxorubicin (Dox) is a chemotherapeutic agent widely used for the treatment of numerous cancers. However, the clinical use of Dox is limited by its unwanted cardiotoxicity. Mitochondrial dysfunction has been associated with Dox-induced cardiotoxicity. To mitigate Dox-related cardiotoxicity, considerable successful examples of a variety of small molecules that target mitochondria to modulate Dox-induced cardiotoxicity have appeared in recent years. Here, we review the related literatures and discuss the evidence showing that mitochondria-targeting small molecules are promising cardioprotective agents against Dox-induced cardiac events. Full article
(This article belongs to the Special Issue Recent Advances in Anticancer Drugs)
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