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Review
. 2023 Dec;38(1):2220084.
doi: 10.1080/14756366.2023.2220084.

Organoboronic acids/esters as effective drug and prodrug candidates in cancer treatments: challenge and hope

Mothana K Al-Omari  1 , Mai Elaarag  2 , Raed M Al-Zoubi  1   2   3 , Ahmad R Al-Qudimat  2 , Ayman A Zarour  4 , Enas A Al-Hurani  5 , Zainab E Fares  3 , Leena M Alkharraz  3 , Mohanad Shkoor  6 , Abdulilah D Bani-Yaseen  6 , Omar M Aboumarzouk  2   7   8 , Aksam Yassin  9 , Abdulla A Al-Ansari  2
Affiliations
Review

Organoboronic acids/esters as effective drug and prodrug candidates in cancer treatments: challenge and hope

Mothana K Al-Omari et al. J Enzyme Inhib Med Chem. 2023 Dec.

Abstract

Boronic acids/esters have recently emerged in the field of medicinal and pharmaceutical research due to their exceptional oxophilicity, low toxicity, and unique structure. They are known as potent enzyme inhibitors, cancer therapy capture agents, and can mimic certain types of antibodies to fight infections. They have been designed and developed into drugs, and this approach has emerged in the last 20 years. Five boronic acid drugs have been approved by the FDA and Health Canada, two of which are used to treat cancer, specifically multiple myeloma. The purpose of this review is to investigate boronic acid/ester derivatives as potential pharmaceutical agents as well as the mechanism of action. It will concentrate on six types of cancer: multiple myeloma, prostate cancer, breast cancer, lung cancer, cervical cancer, and colon cancer. Some newly developed boron-containing compounds have already demonstrated highly promising activities, but further investigation is required before final conclusions can be drawn.

Keywords: Boronic acid; cancer disease; drug; enzyme inhibitor; mechanism.

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Conflict of interest statement

The authors report no conflict of interest.

Figures

None
Graphical abstract
Figure 1.
Figure 1.
The release mechanism of active prodrug from boron-masking using direct C–B bond oxidation/rearrangement strategy.
Figure 2.
Figure 2.
Some biological active organoboron derivatives in medicine.
Figure 3.
Figure 3.
Organoboron derivatives in breast, lung, cervical, and colon cancer treatments.
See this image and copyright information in PMC

References

    1. Watanabe T, Momose I.. [Boronic acid as a promising class of chemical entity for development of clinical medicine for targeted therapy of cancer]. Yakugaku Zasshi. 2022;142(2):145–153. - PubMed
    1. (a) Sun X, Peng Y, Zhao J, Xie Z, Lei X, Tang G.. Discovery and development of tumor glycolysis rate-limiting enzyme inhibitors. Bioorg Chem. 2021;112:104891. - PubMed
    2. (b)Zolghadri S, Bahrami A, Hassan Khan MT, Munoz-Munoz J, Garcia-Molina F, Garcia-Canovas F, Saboury AA.. A comprehensive review on tyrosinase inhibitors. J Enzyme Inhib Med Chem. 2019;34(1):279–309. - PMC - PubMed
    3. (c)Lin H, Li Q, Li Q, Zhu J, Gu K, Jiang X, Hu Q, Feng F, Qu W, Chen Y, et al. . Small molecule KDM4s inhibitors as anti-cancer agents. J Enzyme Inhib Med Chem. 2018;33(1):777–793. - PMC - PubMed
    4. (d)Supuran CT. Anti-obesity carbonic anhydrase inhibitors: challenges and opportunities. J Enzyme Inhib Med Chem. 2022;37(1):2478–2488. - PMC - PubMed
    1. (a) Schwarzel WC, Kruggel WG, Brodie HJ.. Studies on the mechanism of estrogen biosynthesis. 8. The development of inhibitors of the enzyme system in human placenta. Endocrinology. 1973;92(3):866–880. - PubMed
    2. (b)Siiteri PK, Thompson EA.. Studies of human placental aromatase. J Steroid Biochem. 1975;6(3-4):317–322. - PubMed
    3. (c) Brueggemeier RW, Floyd EE, Counsell RE.. Synthesis and biochemical evaluation of inhibitors of estrogen biosynthesis. J Med Chem. 1978;21(10):1007–1011. - PubMed
    1. (a) Lacal PM, Graziani G.. Therapeutic implication of vascular endothelial growth factor receptor-1 (VEGFR-1) targeting in cancer cells and tumor microenvironment by competitive and non-competitive inhibitors. Pharmacol Res. 2018;136:97–107. - PubMed
    2. (b) Zhang Q, Miao YH, Liu T, Yun YL, Sun XY, Yang T, Sun J.. Natural source, bioactivity and synthesis of 3-arylcoumarin derivatives. J Enzyme Inhib Med Chem. 2022;37(1):1023–1042. - PMC - PubMed
    1. McClure JJ, Li X, Chou CJ.. Advances and challenges of HDAC inhibitors in cancer therapeutics. Adv Cancer Res. 2018;138:183–211. - PubMed