Recent developments in the medicinal chemistry of single boron atom-containing compounds

Shu Song; Ping Gao; Lin Sun; Dongwei Kang; Jacob Kongsted; Vasanthanathan Poongavanam; Peng Zhan; Xinyong Liu

doi:10.1016/j.apsb.2021.01.010

Recent developments in the medicinal chemistry of single boron atom-containing compounds

Shu Song
, Ping Gao
, Lin Sun
, Dongwei Kang
, Jacob Kongsted
, Vasanthanathan Poongavanam^*
, Peng Zhan
, Xinyong Liu

^*Corresponding author for this work

Department of Physics, Chemistry and Pharmacy

Shandong University

Research output: Contribution to journal › Journal article › Research › peer-review

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Abstract

Various boron-containing drugs have been approved for clinical use over the past two decades, and more are currently in clinical trials. The increasing interest in boron-containing compounds is due to their unique binding properties to biological targets; for example, boron substitution can be used to modulate biological activity, pharmacokinetic properties, and drug resistance. In this perspective, we aim to comprehensively review the current status of boron compounds in drug discovery, focusing especially on progress from 2015 to December 2020. We classify these compounds into groups showing anticancer, antibacterial, antiviral, antiparasitic and other activities, and discuss the biological targets associated with each activity, as well as potential future developments.

Original language	English
Journal	Acta Pharmaceutica Sinica B
Volume	11
Issue number	10
Pages (from-to)	3035-3059
ISSN	2211-3835
DOIs	https://doi.org/10.1016/j.apsb.2021.01.010
Publication status	Published - Oct 2021

Funding

Financial support from the National Natural Science Foundation of China (No. 81973181 , to Xinyong Liu, China), Shandong Provincial Key Research and Development Project (No. 2019JZZY021011 , to Peng Zhan, China), National Science and Technology Major Projects for “Major New Drugs Innovation and Development” ( 2019ZX09301126 , to Xinyong Liu, China), Outstanding Youth Fund of Shandong Province ( ZR2020JQ31 , to Peng Zhan, China), Foreign Cultural and Educational Experts Project ( GXL20200015001 , to Xinyong Liu, China), the Program for Outstanding Ph.D. Candidate of Shandong University (to Lin Sun, China), Qilu Young Scholars Program of Shandong University (to Peng Zhan, China) and the Taishan Scholar Program at Shandong Province (to Xinyong Liu, China) is gratefully acknowledged.

Keywords

Boron-containing compounds
Covalent inhibitors
Linker components
Prodrug

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title = "Recent developments in the medicinal chemistry of single boron atom-containing compounds",

abstract = "Various boron-containing drugs have been approved for clinical use over the past two decades, and more are currently in clinical trials. The increasing interest in boron-containing compounds is due to their unique binding properties to biological targets; for example, boron substitution can be used to modulate biological activity, pharmacokinetic properties, and drug resistance. In this perspective, we aim to comprehensively review the current status of boron compounds in drug discovery, focusing especially on progress from 2015 to December 2020. We classify these compounds into groups showing anticancer, antibacterial, antiviral, antiparasitic and other activities, and discuss the biological targets associated with each activity, as well as potential future developments.",

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author = "Shu Song and Ping Gao and Lin Sun and Dongwei Kang and Jacob Kongsted and Vasanthanathan Poongavanam and Peng Zhan and Xinyong Liu",

note = "Funding Information: Financial support from the National Natural Science Foundation of China (No. 81973181 , to Xinyong Liu, China), Shandong Provincial Key Research and Development Project (No. 2019JZZY021011 , to Peng Zhan, China), National Science and Technology Major Projects for {\textquotedblleft}Major New Drugs Innovation and Development{\textquotedblright} ( 2019ZX09301126 , to Xinyong Liu, China), Outstanding Youth Fund of Shandong Province ( ZR2020JQ31 , to Peng Zhan, China), Foreign Cultural and Educational Experts Project ( GXL20200015001 , to Xinyong Liu, China), the Program for Outstanding Ph.D. Candidate of Shandong University (to Lin Sun, China), Qilu Young Scholars Program of Shandong University (to Peng Zhan, China) and the Taishan Scholar Program at Shandong Province (to Xinyong Liu, China) is gratefully acknowledged. Publisher Copyright: {\textcopyright} 2021 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences Copyright: Copyright 2021 Elsevier B.V., All rights reserved.",

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AU - Song, Shu

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AU - Poongavanam, Vasanthanathan

AU - Zhan, Peng

AU - Liu, Xinyong

N1 - Funding Information: Financial support from the National Natural Science Foundation of China (No. 81973181 , to Xinyong Liu, China), Shandong Provincial Key Research and Development Project (No. 2019JZZY021011 , to Peng Zhan, China), National Science and Technology Major Projects for “Major New Drugs Innovation and Development” ( 2019ZX09301126 , to Xinyong Liu, China), Outstanding Youth Fund of Shandong Province ( ZR2020JQ31 , to Peng Zhan, China), Foreign Cultural and Educational Experts Project ( GXL20200015001 , to Xinyong Liu, China), the Program for Outstanding Ph.D. Candidate of Shandong University (to Lin Sun, China), Qilu Young Scholars Program of Shandong University (to Peng Zhan, China) and the Taishan Scholar Program at Shandong Province (to Xinyong Liu, China) is gratefully acknowledged. Publisher Copyright: © 2021 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences Copyright: Copyright 2021 Elsevier B.V., All rights reserved.

PY - 2021/10

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N2 - Various boron-containing drugs have been approved for clinical use over the past two decades, and more are currently in clinical trials. The increasing interest in boron-containing compounds is due to their unique binding properties to biological targets; for example, boron substitution can be used to modulate biological activity, pharmacokinetic properties, and drug resistance. In this perspective, we aim to comprehensively review the current status of boron compounds in drug discovery, focusing especially on progress from 2015 to December 2020. We classify these compounds into groups showing anticancer, antibacterial, antiviral, antiparasitic and other activities, and discuss the biological targets associated with each activity, as well as potential future developments.

AB - Various boron-containing drugs have been approved for clinical use over the past two decades, and more are currently in clinical trials. The increasing interest in boron-containing compounds is due to their unique binding properties to biological targets; for example, boron substitution can be used to modulate biological activity, pharmacokinetic properties, and drug resistance. In this perspective, we aim to comprehensively review the current status of boron compounds in drug discovery, focusing especially on progress from 2015 to December 2020. We classify these compounds into groups showing anticancer, antibacterial, antiviral, antiparasitic and other activities, and discuss the biological targets associated with each activity, as well as potential future developments.

KW - Boron-containing compounds

KW - Covalent inhibitors

KW - Linker components

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Recent developments in the medicinal chemistry of single boron atom-containing compounds

Abstract

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