Recent progress in the syntheses and biological evaluation of boronated Porphyrins for boron neutron-capture therapy
Recent progress in the syntheses and biological evaluation of boronated Porphyrins for boron neutron-capture therapy
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DOI：
10.2174/187152006776119135
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发表时间：
2006-03-01
影响因子：
2.8
通讯作者：
Vicente, M. G. H.
中科院分区：
文献类型：
--
作者：
Renner, M. W.;Miura, M.;Vicente, M. G. H.
硼化卟啉是目前正在实验和临床研究的两种癌症双峰疗法中的一类重要肿瘤定位剂;硼中子捕获疗法（BNCT）和光动力疗法（PDT）。硼化卟啉的理想性质是它们是容易合成的、纯的和良好表征的药物，并且在体内，它们是稳定的、肿瘤特异性的，具有高的肿瘤：血液和肿瘤：正常组织硼浓度比，并且引起最小的毒性。本文介绍了大量新的卟啉化合物及其合成。重点是过去5年内发表的卟啉类化合物，但也回顾了过去15年来卟啉类化合物在体内研究的意义和趋势。许多具有相当不寻常的，新的结构和其他附加细胞靶向部分更大的肿瘤特异性。除了常用的closo-和nido-o-碳硼烷，其他硼笼和连接方式。这些硼笼可以选择性地改变卟啉的亲脂性、亲水性和两亲性以及它们的硼含量。新的递送方式也大大提高了以前被认为不适合用于BNCT的化合物的靶向潜力。
Boronated porphyrins are an important class of tumor-localizing agents in two bimodal therapies for cancer currently under study experimentally and clinically; boron neutron-capture therapy (BNCT) and photodynamic therapy (PDT). The desirable properties for the boronated porphyrins are that they are easily synthesized, pure and well-characterized drugs, and that in vivo, they are stable, tumor-specific, with high tumor: blood and tumor: normal tissue boron concentration ratios, and cause minimal toxicity. A large number of new porphyrins and their syntheses are presented herein. The focus is primarily on porphyrins published within the past 5 years, but the implications and trends from porphyrins studied in vivo over the past 15 years are also reviewed. Many possess quite unusual, novel structures and others have appended cell-targeting moieties for greater tumor specificity. Besides the commonly used closo- and nido-o-carboranes other boron cages and modes of attachment are presented. These boron cages can selectively alter the lipophilic, hydrophilic and amphiphilic properties of the porphyrins as well as their boron content. New delivery modalities have also greatly improved the targeting potential of compounds previously deemed unsuitable for applications in BNCT.