Selective boron drug delivery to brain tumors for boron neutron capture therapy

Chen, Wei; Mehta, Samir C.; Lü, Donghao

doi:10.1016/s0169-409x(97)00037-9

Cited by 79 publications

(39 citation statements)

References 96 publications

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“…[49] Finally, boron-containing molecules, including boronic acids and carboranes, [50] have long been investigated as agents for boron-neutron capture therapy (BCNT) for the treatment of tumours. [37,50,51] …”

Section: Biological and Medicinal Applicationsmentioning

confidence: 99%

Expanding Roles for Organoboron Compounds – Versatile and Valuable Molecules for Synthetic, Biological and Medicinal Chemistry

Petasis

2007

Aust. J. Chem.

109

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The present essay offers an overview of the latest developments in the chemistry of organoboron compounds. The unique structural characteristics and the versatile reactivity profile of organoboron compounds continue to expand their roles in several areas of chemistry. A growing number of boron-mediated reactions have become vital tools for synthetic chemistry, particularly in asymmetric synthesis, metal-catalyzed processes, acid catalysis, and multicomponent reactions. As a result, boronic acids and related molecules have now evolved as major players in synthetic and medicinal chemistry. Moreover, their remnant electrophilic reactivity, even under physiological conditions, has allowed their incorporation in a growing number of bioactive molecules, including bortezomib, a clinically approved anticancer agent. Finally, the sensitive and selective binding of boronic acids to diols and carbohydrates has led to the development of a growing number of novel chemosensors for the detection, quantification, and imaging of glucose and other carbohydrates. There is no doubt that the chemistry of organoboron compounds will continue to expand into new discoveries and new applications in several fields of science. Long History -Expanding RolesOrganic compounds containing boron have been known for over a century, and many aspects of their chemical properties and reactivity have been known for quite some time. Since the discovery and development of hydroboration, the resulting organoboranes are among the most widely used reagents and intermediates in organic synthesis including asymmetric reactions. Also, early investigations on the chemistry of boron hydrides and carboranes revealed new classes of compounds with unique structure and reactivity that continue to attract attention. Despite these early discoveries, however, the real potential of some of the more versatile and chemically stable organoboron compounds was not realized until recently.Indeed, the growing list of valuable organoboron compounds in addition to organoboranes [1] now includes organoboronic acids and boronates, [2] and more recently organotrifluoroborates.

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Section: Biological and Medicinal Applicationsmentioning

confidence: 99%

Expanding Roles for Organoboron Compounds – Versatile and Valuable Molecules for Synthetic, Biological and Medicinal Chemistry

Petasis

2007

Aust. J. Chem.

109

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“…Using primary cultured bovine brain capillary endothelial cells, Tsuji et al [5,6] have found that P-glycoprotein (ABCB1) acts as an efflux pump for the anti-cancer drugs, vincristine, at the BBB. Schinkel et al [7][8][9] have developed the mdr 1a gene knockout mouse and proved that P-glycoprotein (ie, mdr 1a gene products) plays a key role in restricting the apparent cerebral distributed vinblastine (a substrate of P-glycoprotein) across the BBB. However, several hydrophilic substrates such as metabolites of cerebral neurotransmitters are present in the brain, which reduce the cerebral concentration, and as a result, could play an important role in CNS detoxification.…”

Section: Introductionmentioning

confidence: 99%

Predictive model of blood-brain barrier penetration of organic compounds1

Chen

Yang

2005

Acta Pharmacologica Sinica

190

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Aim: To build up a theoretical model of organic compounds for the prediction of the activity of small molecules through the blood‐brain barrier (BBB) in drug design. Methods: A training set of 37 structurally diverse compounds was used to construct quantitative structure‐activity relationship (QSAR) models. Intermolecular and intramolecular solute descriptors were calculated using molecular mechanics, molecular dynamics simulations, quantum chemistry and so on. The QSAR models were optimized using multidimensional linear regression fitting and stepwise method. A test set of 8 compounds was evaluated using the models as part of a validation process. Results: Significant QSAR models (R=0.955, s=0.232) of the BBB penetration of organic compounds were constructed. BBB penetration was found to depend upon the polar surface area, the octanol/water partition coefficient, Balaban Index, the strength of a small molecule to combine with the membrane‐water complex, and the changeability of the structure of a solute‐membrane‐water complex. Conclusion: The QSAR models indicate that the distribution of organic molecules through BBB is not only influenced by organic solutes themselves, but also relates to the properties of the solute‐membrane‐water complex, that is, interactions of the molecule with the phospholipid‐rich regions of cellular membranes.

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“…this purpose is 10 B and in such case the therapy is called BNCT (Boron Neutron Capture Therapy) [120,121]. The suitable carrier (such as liposome [120,121] or boron nitride nanotubes [122] or nanoparticles [123]) preconcentrates the target nuclide in tumor tissue {first targeting) and then narrow neutron beam is focused to the lesion {second targeting). The method, although undoubtedly elegant, possess some drawbacks.…”

Section: Minimization Of Systemic Radiation Burdenmentioning

confidence: 99%

Nano‐sized Carrier Systems as New Materials for Nuclear Medicine

Hrubý

2012

Intelligent Nanomaterials

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Materials with nano-sized architecture currenly attract a lot of attention for various applications because they possess many unique properties. Several of the currently most studied applications of nanotechnology are in medicine, especially in the delivery of chemical drugs, and also in nuclear medicine, which is the focus of this review. The main areas of interest for nano-sized systems exploitable in nuclear medicine are imaging of reticuloendothelial system by single photon emission tomography, radiosynovectomy with beta-emitter-labeled particles, and diagnostic or therapeutic cancer applications exploiting passive targeting of radionuclides to solid tumors by enhanced permeation and retention (EPR) effect, or by active targeting approaches.

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Selective boron drug delivery to brain tumors for boron neutron capture therapy

Cited by 79 publications

References 96 publications

Expanding Roles for Organoboron Compounds – Versatile and Valuable Molecules for Synthetic, Biological and Medicinal Chemistry

Expanding Roles for Organoboron Compounds – Versatile and Valuable Molecules for Synthetic, Biological and Medicinal Chemistry

Predictive model of blood-brain barrier penetration of organic compounds1

Nano‐sized Carrier Systems as New Materials for Nuclear Medicine

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