Boron-Based Compounds最新文献_第2页

Twenty Years of Research on 3-Carboranyl Thymidine Analogs (3CTAs) 3-碳硼基胸苷类似物(3cta)的二十年研究

Boron-Based Compounds Pub Date : 2018-07-12 DOI: 10.1002/9781119275602.CH3.1

W. Tjarks

引用次数: 0

Boron Compounds in Molecular Imaging 硼化合物在分子成像中的应用

Boron-Based Compounds Pub Date : 2018-07-12 DOI: 10.1002/9781119275602.CH2.4

B. Das, D. P. Ojha, Sasmita Das, Todd Evans

引用次数: 3

Optimizing the Therapeutic Efficacy of Boron Neutron Capture Therapy (BNCT) for Different Pathologies 优化硼中子俘获疗法(BNCT)对不同病理的疗效

Boron-Based Compounds Pub Date : 2018-07-12 DOI: 10.1002/9781119275602.CH3.6

A. Schwint, A. M. Hughes, M. A. Garabalino, E. Pozzi, E. Heber, V. Trivillin

引用次数: 0

Index 指数

Boron-Based Compounds Pub Date : 2018-07-12 DOI: 10.1002/9781119275602.index

引用次数: 0

Half- and Mixed-Sandwich Transition Metal Dicarbollides andnido-Carboranes(-1) for Medicinal Applications 医药用半和混合夹层过渡金属二碳内酯和烯多碳硼烷(-1)

Boron-Based Compounds Pub Date : 2018-07-12 DOI: 10.1002/9781119275602.CH1.4

B. Schwarze, M. Gozzi, E. Hey‐Hawkins

{"title":"Half- and Mixed-Sandwich Transition Metal Dicarbollides andnido-Carboranes(-1) for Medicinal Applications","authors":"B. Schwarze, M. Gozzi, E. Hey‐Hawkins","doi":"10.1002/9781119275602.CH1.4","DOIUrl":"https://doi.org/10.1002/9781119275602.CH1.4","url":null,"abstract":"Today, medicinal chemistry is still clearly dominated by organic chemistry, and most of the marketed drugs are purely organic molecules that can incorporate nitrogen, oxygen, and halogens besides carbon and hydrogen. On the other hand, commercial boron‐ based drugs are still rare [1]. Besides bortezomib, tavaborole (AN2690), crisaborole (AN2728), epetraborole (AN3365), and SCYX‐7158 (AN5568) [2], l‐4‐(dihydroxybo ryl)phenylalanine (BPA) and sodium mercapto‐undecahydro‐closo‐dodecaborate (BSH) are used as drugs in boron neutron capture therapy (BNCT) [3–5]. Like carbon, boron readily forms compounds with covalent boron–hydrogen bonds and also boron–boron interactions. However, in contrast to hydrocarbons, boranes prefer the formation of polyhedral clusters with fascinating globular architectures [6]. Most boranes are unstable in aqueous environment; an exception is closo‐B12H12. In contrast, polyhedral carboranes, in which two BH– units of closo‐B12H12 are replaced by two CH vertices (closo‐C2B10H12, dicarba‐closo‐dodecaborane(12), carborane or carbaborane), have remarkable biological stability. Furthermore, the two carbon atoms are versatile starting points for various organic modifications. Carboranes are of special interest due to their unique properties that cannot be found in organic counterparts. These unique properties are based on the element boron, due to its inherent electron deficiency, lower electronegativity, and smaller orbital size compared to carbon. Of the borane clusters and heteroboranes, the three dicarba‐closo‐dodecaborane(12) isomers (ortho (1,2‐), meta (1,7‐), and para (1,12‐dicarba‐closo‐dodecaborane(12)), each of which has specific electronic properties, have attracted much interest. Besides the use Half‐ and Mixed‐Sandwich Transition Metal Dicarbollides and nido‐Carboranes(–1) for Medicinal Applications Benedikt Schwarze, Marta Gozzi, and Evamarie Hey‐Hawkins*","PeriodicalId":124832,"journal":{"name":"Boron-Based Compounds","volume":"87 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2018-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114722290","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 4

Carborane Derivatives of Porphyrins and Chlorins for Photodynamic and Boron Neutron Capture Therapies 用于光动力和硼中子捕获治疗的卟啉和氯的碳硼烷衍生物

Boron-Based Compounds Pub Date : 2018-07-12 DOI: 10.1002/9781119275602.CH3.3

V. Ol’shevskaya, Andrei V. Zaitsev, A. Shtil

引用次数: 4

Design of Carborane-Based Hypoxia-Inducible Factor Inhibitors 碳硼烷类缺氧诱导因子抑制剂的设计

Boron-Based Compounds Pub Date : 2018-07-12 DOI: 10.1002/9781119275602.CH1.3

Guangzhe Li, H. Ban, Hiroyuki Nakamura

{"title":"Design of Carborane-Based Hypoxia-Inducible Factor Inhibitors","authors":"Guangzhe Li, H. Ban, Hiroyuki Nakamura","doi":"10.1002/9781119275602.CH1.3","DOIUrl":"https://doi.org/10.1002/9781119275602.CH1.3","url":null,"abstract":"Cancer is a disease involving uncontrolled cell growth. In a solid tumor, cancer cells are deprived of oxygen due to their rapid growth. As a result, the oxygen concentration of the tumor regions distant from blood vessels is significantly lower than that of healthy tissues, causing hypoxia in tumor. Tumor hypoxia upregulates a number of genes involved in tumor angiogenesis, cellular energy metabolism, metastasis, cell prolifera‐ tion, and resistance to apoptosis. Hypoxia‐inducible factor (HIF) is a transcriptional factor that plays an important role as an oxygen sensor in cells. HIF is a heterodimer composed of α subunits (HIF1α, ‐2α, and ‐3α) and a β subunit (HIF1β, which is also known as an aryl hydrocarbon receptor nuclear translocator [ARNT]) [1,2]. Under aerobic conditions, posttranslational hydroxylation of proline residues in HIF1α by prolyl hydroxylase (PHD) induces ubiquitination by the von Hippel–Lindau (VHL) tumor suppressor protein, a component of the E3 ubiquitin ligase complex, resulting in the oxygen‐dependent degradation through a ubiquitin– proteasome pathway. Under hypoxic conditions, HIF1α does not undergo the oxygen‐dependent degradation due to the inactivation of PHD; instead, it translocates into the nucleus, where it dimerizes with the constitutively expressed HIF1β to form a heterodimeric complex. HIF binds to the hypoxia response element (HRE) DNA sequence with co‐activators to activate various genes, including glucose transporters, glycolytic enzymes, angiogenic growth factors, and several molecules involved in apoptosis and cell proliferation [3,4]. The activated HIF plays pivotal roles in various pathological conditions, including inflammation, cardiovascular disorder, and cancer. Indeed, overexpression of HIF1α has been observed in human cancers, including brain, breast, colon, lung, ovary, and prostate cancers [5]; thus, HIF1α is a novel target of cancer therapy. We have studied a boron‐based medicinal drug design. A boron atom has a vacant orbital and readily interconverts between the neutral sp2 and anionic sp3 hybridization Design of Carborane‐Based Hypoxia‐Inducible Factor Inhibitors Guangzhe Li, Hyun Seung Ban, and Hiroyuki Nakamura","PeriodicalId":124832,"journal":{"name":"Boron-Based Compounds","volume":"2 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2018-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"122119992","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1