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硼化学在诊断和治疗中的应用。

Boron chemicals in diagnosis and therapeutics.

机构信息

Division of Hematology & Oncology, Department of Internal Medicine, Kansas University Medical Center, Kansas City, KS 66103, USA.

出版信息

Future Med Chem. 2013 Apr;5(6):653-76. doi: 10.4155/fmc.13.38.

DOI:10.4155/fmc.13.38
PMID:23617429
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3703777/
Abstract

Advances in the field of boron chemistry have expanded the application of boron from material use to medicine. Boron-based drugs represent a new class of molecules that possess several biomedical applications including use as imaging agents for both optical and nuclear imaging as well as therapeutic agents with anticancer, antiviral, antibacterial, antifungal and other disease-specific activities. For example, bortezomib (Velcade(®)), the only drug in clinical use with boron as an active element, was approved in 2003 as a proteasome inhibitor for the treatment of multiple myeloma and non-Hodgkin's lymphoma. Several other boron-based compounds are in various phases of clinical trials, which illustrates the promise of this approach for medicinal chemists working in the area of boron chemistry. It is expected that in the near future, several boron-containing drugs should become available in the market with better efficacy and potency than existing drugs. This article discusses the current status of the development of boron-based compounds as diagnostic and therapeutic agents in humans.

摘要

硼化学领域的进展将硼的应用从材料用途扩展到了医学领域。基于硼的药物代表了一类新的分子,具有多种生物医学应用,包括用作光学和核成像的造影剂以及具有抗癌、抗病毒、抗菌、抗真菌和其他特定疾病活性的治疗剂。例如,硼替佐米(硼替佐米),是唯一一种临床应用中含有硼作为活性元素的药物,于 2003 年被批准为蛋白酶体抑制剂,用于治疗多发性骨髓瘤和非霍奇金淋巴瘤。还有其他几种基于硼的化合物处于不同的临床试验阶段,这说明了硼化学领域的药物化学家在这一方法上的前景。预计在不久的将来,几种含硼药物将在市场上推出,其疗效和效力将优于现有药物。本文讨论了硼化合物作为诊断和治疗人类疾病的试剂的发展现状。

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Boron-Based 4-Hydroxytamoxifen Bioisosteres for Treatment of de Novo Tamoxifen Resistant Breast Cancer.用于治疗原发性他莫昔芬耐药乳腺癌的硼基4-羟基他莫昔芬生物电子等排体
ACS Med Chem Lett. 2012 Apr 6;3(5):392-396. doi: 10.1021/ml3000287.
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Design and synthesis of boron containing potential pan-RAR inverse agonists.
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