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

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

Institution:	1. Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Ji''nan 250012, China;2. Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Odense M. DK-5230, Denmark

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.

Keywords:	Boron-containing compounds Covalent inhibitors Prodrug Linker components ACTs"} {"#name":"keyword" "$":{"id":"kwrd0035"} "$$":[{"#name":"text" "_":"artemisinin combination therapies ADCs"} {"#name":"keyword" "$":{"id":"kwrd0045"} "$$":[{"#name":"text" "$$":[{"#name":"italic" "_":"Acinetobacter"} {"#name":"__text__" "_":"-derived cephalosporinases AML"} {"#name":"keyword" "$":{"id":"kwrd0055"} "$$":[{"#name":"text" "_":"acute myeloid leukemia AMT"} {"#name":"keyword" "$":{"id":"kwrd0065"} "$$":[{"#name":"text" "_":"aminopterin BLs"} {"#name":"keyword" "$":{"id":"kwrd0075"} "$$":[{"#name":"text" "$$":[{"#name":"italic" "_":"β"} {"#name":"__text__" "_":"-lactamases BNCT"} {"#name":"keyword" "$":{"id":"kwrd0085"} "$$":[{"#name":"text" "_":"boron neutron capture therapy BNNPs"} {"#name":"keyword" "$":{"id":"kwrd0095"} "$$":[{"#name":"text" "_":"boron nitride nanoparticles BNNTs"} {"#name":"keyword" "$":{"id":"kwrd0105"} "$$":[{"#name":"text" "_":"boron nitride nanotubes CEs"} {"#name":"keyword" "$":{"id":"kwrd0115"} "$$":[{"#name":"text" "_":"carboxylesterases CIA"} {"#name":"keyword" "$":{"id":"kwrd0125"} "$$":[{"#name":"text" "_":"collagen-induced arthritis ClpP"} {"#name":"keyword" "$":{"id":"kwrd0135"} "$$":[{"#name":"text" "_":"casein protease P COVID-19"} {"#name":"keyword" "$":{"id":"kwrd0145"} "$$":[{"#name":"text" "_":"coronavirus disease 2019 cUTI"} {"#name":"keyword" "$":{"id":"kwrd0155"} "$$":[{"#name":"text" "_":"complex urinary tract infection dCTPase"} {"#name":"keyword" "$":{"id":"kwrd0165"} "$$":[{"#name":"text" "_":"dCTPase pyrophosphatase GSH"} {"#name":"keyword" "$":{"id":"kwrd0175"} "$$":[{"#name":"text" "_":"glutathione HADC1"} {"#name":"keyword" "$":{"id":"kwrd0185"} "$$":[{"#name":"text" "_":"class I histone deacetylase HBV"} {"#name":"keyword" "$":{"id":"kwrd0195"} "$$":[{"#name":"text" "_":"hepatitis B virus HCV"} {"#name":"keyword" "$":{"id":"kwrd0205"} "$$":[{"#name":"text" "_":"hepatitis C virus HIV"} {"#name":"keyword" "$":{"id":"kwrd0215"} "$$":[{"#name":"text" "_":"human immunodeficiency virus LeuRS"} {"#name":"keyword" "$":{"id":"kwrd0225"} "$$":[{"#name":"text" "_":"leucyl-tRNA synthetase MBLs"} {"#name":"keyword" "$":{"id":"kwrd0235"} "$$":[{"#name":"text" "$$":[{"#name":"__text__" "_":"metal "} {"#name":"italic" "_":"β"} {"#name":"__text__" "_":"-lactamases Mcl-1"} {"#name":"keyword" "$":{"id":"kwrd0245"} "$$":[{"#name":"text" "_":"myeloid cell leukemia 1 MDR-TB"} {"#name":"keyword" "$":{"id":"kwrd0255"} "$$":[{"#name":"text" "_":"multidrug-resistant tuberculosis MERS"} {"#name":"keyword" "$":{"id":"kwrd0265"} "$$":[{"#name":"text" "_":"Middle East respiratory syndrome MIDA"} {"#name":"keyword" "$":{"id":"kwrd0275"} "$$":[{"#name":"text" "$$":[{"#name":"italic" "_":"N"} {"#name":"__text__" "_":"-methyliminodiacetic acid MM"} {"#name":"keyword" "$":{"id":"kwrd0285"} "$$":[{"#name":"text" "_":"multiple myeloma Mtb"} {"#name":"keyword" "$":{"id":"kwrd0295"} "$$":[{"#name":"text" "$$":[{"#name":"italic" "_":"Mycobacterium tuberculosis MTX"} {"#name":"keyword" "$":{"id":"kwrd0305"} "$$":[{"#name":"text" "_":"methotrexate NA"} {"#name":"keyword" "$":{"id":"kwrd0315"} "$$":[{"#name":"text" "_":"neuraminidase NS5B"} {"#name":"keyword" "$":{"id":"kwrd0325"} "$$":[{"#name":"text" "_":"non-nucleoside polymerase OBORT"} {"#name":"keyword" "$":{"id":"kwrd0335"} "$$":[{"#name":"text" "_":"oxaborole tRNA capture QM"} {"#name":"keyword" "$":{"id":"kwrd0345"} "$$":[{"#name":"text" "_":"quinone methide OPs"} {"#name":"keyword" "$":{"id":"kwrd0355"} "$$":[{"#name":"text" "_":"organophosphate PBA"} {"#name":"keyword" "$":{"id":"kwrd0365"} "$$":[{"#name":"text" "_":"phenylboronic acid PDB"} {"#name":"keyword" "$":{"id":"kwrd0375"} "$$":[{"#name":"text" "_":"Protein Data Bank PPI"} {"#name":"keyword" "$":{"id":"kwrd0385"} "$$":[{"#name":"text" "_":"protein–protein interaction RA"} {"#name":"keyword" "$":{"id":"kwrd0395"} "$$":[{"#name":"text" "_":"rheumatoid arthritis ROS"} {"#name":"keyword" "$":{"id":"kwrd0405"} "$$":[{"#name":"text" "_":"reactive oxygen species SARS-CoV-2"} {"#name":"keyword" "$":{"id":"kwrd0425"} "$$":[{"#name":"text" "_":"syndrome coronavirus 2 SBLs"} {"#name":"keyword" "$":{"id":"kwrd0435"} "$$":[{"#name":"text" "$$":[{"#name":"__text__" "_":"serine "} {"#name":"italic" "_":"β"} {"#name":"__text__" "_":"-lactamases SERD"} {"#name":"keyword" "$":{"id":"kwrd0445"} "$$":[{"#name":"text" "_":"selective estrogen receptor downregulator SHA"} {"#name":"keyword" "$":{"id":"kwrd0455"} "$$":[{"#name":"text" "_":"salicyl hydroxamic acid TB"} {"#name":"keyword" "$":{"id":"kwrd0465"} "$$":[{"#name":"text" "_":"tuberculosis TTR"} {"#name":"keyword" "$":{"id":"kwrd0475"} "$$":[{"#name":"text" "_":"transthyretin U4CR"} {"#name":"keyword" "$":{"id":"kwrd0485"} "$$":[{"#name":"text" "_":"Ugi 4-component reaction
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