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Pharmaceuticals
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Boron in Medicinal Chemistry: From Synthesis to Therapeutic Applications
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Boron in Medicinal Chemistry: From Synthesis to Therapeutic Applications

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

Deadline for manuscript submissions: 25 August 2024 | Viewed by 4057

Special Issue Editors

Dr. Daniela Imperio

E-Mail Website
Guest Editor
Department of Pharmaceutical Sciences, University of Piemonte Orientale, 28100 Novara, Italy
Interests: carbohydrates; boronic acids; benzoxaboroles; boron clusters; BNCT
Prof. Dr. Luigi Panza

E-Mail Website
Guest Editor
Department of Pharmaceutical Sciences, University of Piemonte Orientale, 28100 Novara, Italy
Interests: carbohydrates; boronic acids; benzoxaboroles; boron clusters; BNCT

Special Issue Information

Dear colleagues,

In recent years, the interest in boron-based compounds for medical applications has grown significantly, bearing the development of new drugs, e.g., Velcade® (bortezomib), which is used in the treatment of multiple myeloma. This Special Issue is dedicated to all aspects of boron-based compounds with potential pharmaceutical interest, including clusters of boron (carboranes, metallaboranes, metallacarboranes, aminoboranes, etc.), organic and bio-organic boron conjugates (boronic acids and their complexes as well as derivatives, benzoxaboroles), and boron in materials (including polymers and dendrimers), that can have an impact on the medical field, with anticancer, bactericidal, antifungal, and anti-HIV activity, anti-rheumatoid arthritis activity, applications of boron in drug delivery and imaging for diagnosis, or compounds focused on boron neutron capture therapy.

It is a pleasure to invite you to submit a manuscript to this Special Issue; regular articles, communications, and reviews are all welcome.

Dr. Daniela Imperio
Prof. Dr. Luigi Panza
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. 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

  • boronic acids
  • benzoxaboroles
  • boron clusters
  • carboranes
  • boron neutron capture therapy
  • boron-based drugs
  • drug design
  • boron delivery agents
  • medical applications
 
 
 
 
 
 

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Published Papers (3 papers)

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Research

15 pages, 3671 KiB  
Article
One-Step Synthesis, Crystallography, and Acute Toxicity of Two Boron–Carbohydrate Adducts That Induce Sedation in Mice
by Ricardo Ivan Cordova-Chávez, José G. Trujillo-Ferrara, Itzia I. Padilla-Martínez, Héctor González-Espinosa, Antonio Abad-García, Eunice D. Farfán-García, Clara Ortega-Camarillo, Alejandra Contreras-Ramos and Marvin A. Soriano-Ursúa
Pharmaceuticals 2024, 17(6), 781; https://doi.org/10.3390/ph17060781 - 14 Jun 2024
Viewed by 1124
Abstract
Boronic acids form diester bonds with cis-hydroxyl groups in carbohydrates. The formation of these adducts could impair the physical and chemical properties of precursors, even their biological activity. Two carbohydrate derivatives from d-fructose and d-arabinose and phenylboronic acid were synthesized in [...] Read more.
Boronic acids form diester bonds with cis-hydroxyl groups in carbohydrates. The formation of these adducts could impair the physical and chemical properties of precursors, even their biological activity. Two carbohydrate derivatives from d-fructose and d-arabinose and phenylboronic acid were synthesized in a straightforward one-step procedure and chemically characterized via spectroscopy and X-ray diffraction crystallography. Additionally, an acute toxicity test was performed to determine their lethal dose 50 (LD50) values by using Lorke’s method. Analytical chemistry assays confirmed the formation of adducts by the generation of diester bonds with the β-d-pyranose of carbohydrates, including signals corresponding to the formation of new bonds, such as the stretching of B–O bonds. NMR spectra yielded information about the stereoselectivity in the synthesis reaction: Just one signal was found in the range for the anomeric carbon in the 13C NMR spectra of both adducts. The acute toxicity tests showed that the LD50 value for both compounds was 1265 mg/kg, while the effective dose 50 (ED50) for sedation was 531 mg/kg. However, differences were found in the onset and lapse of sedation. For example, the arabinose derivative induced sedation for more than 48 h at 600 mg/kg, while the fructose derivative induced sedation for less than 6 h at the same dose without the death of the mice. Thus, we report for the first time two boron-containing carbohydrate derivatives inducing sedation after intraperitoneal administration. They are bioactive and highly safe agents. Further biological evaluation is desirable to explore their medical applications. Full article
(This article belongs to the Special Issue Boron in Medicinal Chemistry: From Synthesis to Therapeutic Applications)
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13 pages, 5228 KiB  
Article
PK Modeling of L-4-Boronophenylalanine and Development of Bayesian Predictive Platform for L-4-Boronophenylalanine PKs for Boron Neutron Capture Therapy
by Woohyoung Kim, Ji Yeong Won, Jungyu Yi, Seung Chan Choi, Sang Min Lee, Kyungran Mun and Hyeong-Seok Lim
Pharmaceuticals 2024, 17(3), 301; https://doi.org/10.3390/ph17030301 - 26 Feb 2024
Viewed by 955
Abstract
L-4-[(10B)]Boronophenylalanine (BPA) is an amino acid analogue with a boron-10 moiety. It is most widely used as a boron carrier in boron neutron capture therapy. In this study, a Bayesian predictive platform of blood boron concentration based on a BPA pharmacokinetic [...] Read more.
L-4-[(10B)]Boronophenylalanine (BPA) is an amino acid analogue with a boron-10 moiety. It is most widely used as a boron carrier in boron neutron capture therapy. In this study, a Bayesian predictive platform of blood boron concentration based on a BPA pharmacokinetic (PK) model was developed. This platform is user-friendly and can predict the individual boron PK and optimal time window for boron neutron capture therapy in a simple way. The present study aimed to establish a PK model of L-4-boronophenylalanine and develop a Bayesian predictive platform for blood boron PKs for user-friendly estimation of boron concentration during neutron irradiation of neutron capture therapy. Whole blood boron concentrations from seven previous reports were graphically extracted and analyzed using the nonlinear mixed-effects modeling (NONMEM) approach. Model robustness was assessed using nonparametric bootstrap and visual predictive check approaches. The visual predictive check indicated that the final PK model is able to adequately predict observed concentrations. The Shiny package was used to input real-time blood boron concentration data, and during the following irradiation session blood boron was estimated with an acceptably short calculation time for the determination of irradiation time. Finally, a user-friendly Bayesian estimation platform for BPA PKs was developed to optimize individualized therapy for patients undergoing BNCT. Full article
(This article belongs to the Special Issue Boron in Medicinal Chemistry: From Synthesis to Therapeutic Applications)
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12 pages, 1162 KiB  
Article
Carborane-Based ABCG2-Inhibitors Sensitize ABC-(Over)Expressing Cancer Cell Lines for Doxorubicin and Cisplatin
by Svetlana Paskas, Philipp Stockmann, Sanja Mijatović, Lydia Kuhnert, Walther Honscha, Evamarie Hey-Hawkins and Danijela Maksimović-Ivanić
Pharmaceuticals 2023, 16(11), 1582; https://doi.org/10.3390/ph16111582 - 9 Nov 2023
Viewed by 1205
Abstract
The ABCG2 transporter protein, as part of several known mechanisms involved in multidrug resistance, has the ability to transport a broad spectrum of substrates out of the cell and is, therefore, considered as a potential target to improve cancer therapies or as an [...] Read more.
The ABCG2 transporter protein, as part of several known mechanisms involved in multidrug resistance, has the ability to transport a broad spectrum of substrates out of the cell and is, therefore, considered as a potential target to improve cancer therapies or as an approach to combat drug resistance in cancer. We have previously reported carborane-functionalized quinazoline derivatives as potent inhibitors of human ABCG2 which effectively reversed breast cancer resistance protein (BCRP)-mediated mitoxantrone resistance. In this work, we present the evaluation of our most promising carboranyl BCRP inhibitors regarding their toxicity towards ABCG2-expressing cancer cell lines (MCF-7, doxorubicin-resistant MCF-7 or MCF-7 Doxo, HT29, and SW480) and, consequently, with the co-administration of an inhibitor and therapeutic agent, their ability to increase the efficacy of therapeutics with the successful inhibition of ABCG2. The results obtained revealed synergistic effects of several inhibitors in combination with doxorubicin or cisplatin. Compounds DMQCa, DMQCc, and DMQCd showed a decrease in IC50 value in ABCB1- and ABCG2-expressing SW480 cells, suggesting a possible targeting of both transporters. In an HT29 cell line, with the highest expression of ABCG2 among the tested cell lines, using co-treatment of doxorubicin and DMQCd, the effective inhibitory concentration of the antineoplastic agent could be reduced by half. Interestingly, co-treatment of compound QCe with cisplatin, which is not an ABCG2 substrate, showed synergistic effects in MCF-7 Doxo and HT29 cells (IC50 values halved or reduced by 20%, respectively). However, a literature-known upregulation of cisplatin-effluxing ABC transporters and their effective inhibition by the carborane derivatives emerges as a possible reason. Full article
(This article belongs to the Special Issue Boron in Medicinal Chemistry: From Synthesis to Therapeutic Applications)
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Planned Papers

The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.

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