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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

Turning Fear of Boron Toxicity into Boron-containing Drug Design

Author(s): Marvin A. Soriano-Ursúa *, Eunice D. Farfán-García and Simonetta Geninatti-Crich

Volume 26, Issue 26, 2019

Page: [5005 - 5018] Pages: 14

DOI: 10.2174/0929867326666190327154954

Price: $65


Background: Despite the historical employment of boron-containing compounds (BCCs) with medicinal purposes, the reported cases of BCC toxicity in humans during the twentieth-century drived us towards a “boron-withdrawal” period. Fortunately, the use of boric acid for specific purposes remains, and the discovery of natural BCCs with biological action attractive for therapeutic purposes as well as the introduction of some new BCCs for clinical use has reactivated the interest in studying the properties of these BCCs.

Methods: We carried out a structured search of bibliographic databases for scientific peerreviewed research literature regarding boron toxicity and linked that information to that of BCCs in drug design and development. A deductive qualitative content analysis methodology was applied to analyse the interventions and findings of the included studies using a theoretical outline.

Results: This review recapitulates the following on a timeline: the boron uses in medicine, the data known about the toxicological profiles of some BCCs, the pharmacological properties of some BCCs that are employed in cancer and infectious disease therapies, and the known properties of BCCs recently introduced into clinical assays as well as the identification of their structure-activity relationships for toxicity and therapeutic use. Then, we discuss the use of new approaches taking advantage of some toxicological data to identify potent and efficient BCCs for prevention and therapy while limiting their toxic effects.

Conclusion: Data for boron toxicity can be strategically used for boron-containing drug design.

Keywords: Boron, boron-containing compounds, structure-toxicity relationship, drug design, toxicology, infectious disease therapies.

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