Abstract:
:Eldecalcitol [1α,25-dihydroxy-2β-(3-hydroxypropoxy)vitamin D(3)], an analog of calcitriol (1α,25-dihydroxyvitamin D(3)), possesses a hydroxypropoxy substituent at the 2β-position of calcitriol. Eldecalcitol has potent biological effects on bone disease such as osteoporosis. The marketing of eldecalcitol has very recently started in Japan. In consideration of this, we have been investigating practical synthesis of eldecalcitol for industrial-scale production. Eldecalcitol was initially synthesized in a linear manner. The 27-step linear sequence was, however, suboptimal due to its lengthiness and low overall yield (ca. 0.03%). Next, we developed a convergent approach based on the Trost coupling reaction, in which the A-ring fragment (ene-yne part obtained in 10.4% overall yield) and the C/D-ring fragment (bromomethylene part obtained in 27.1% overall yield) are coupled to produce the triene system of eldecalcitol (15.6%). Although the overall yield of the convergent synthesis was better than that of the linear synthesis, significant improvements were still necessary. Therefore, additional biomimetic studies were investigated. Process development for the practical production of eldecalcitol is described herein.
journal_name
Anticancer Resjournal_title
Anticancer researchauthors
Kubodera N,Hatakeyama Ssubject
Has Abstractpub_date
2012-01-01 00:00:00pages
303-9issue
1eissn
0250-7005issn
1791-7530pii
32/1/303journal_volume
32pub_type
杂志文章abstract:BACKGROUND/AIM:We evaluated the efficacy and safety of carbon-ion radiotherapy (CIRT) alone for Stage III non-small-cell lung cancer (NSCLC). PATIENTS AND METHODS:Data of 65 patients (median age=73 years) with Stage III NSCLC who underwent CIRT alone in the QST Hospital, Chiba, Japan, between 1997 and 2015 were retros...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.13963
更新日期:2020-01-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
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abstract::E-selectin which is expressed on endothelial cells plays an important role in the adhesion of cancer cells to the vascular endothelium, being the ligand for a carbohydrate antigen expressed on cancer cells. In this study, the clinical usefulness of this protein was examined. E-selectin was expressed on the endothelial...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2000-09-01 00:00:00
abstract:PURPOSE:To investigate the differences between two rat yolk sac tumor cell lines with different radiosensitivities in etoposide sensitivity and in the sensitizing effect of etoposide in combination with irradiation. MATERIALS AND METHODS:NMT-1 is a parent radiosensitive cell line and NMT-1R is a variant radioresistant...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2003-07-01 00:00:00
abstract:UNLABELLED:The aim this study was to assess the efficacy of cisplatin-epirubicin-vinorelbine, as primary chemotherapy, in reducing the tumour burden in T2-3 N0-2 breast carcinomas. Breast conservative surgery (BCS) rate, clinical and pathological complete response (pCR), toxicity and 5-year disease-free survival (DFS) ...
journal_title:Anticancer research
pub_type: 杂志文章,多中心研究
doi:
更新日期:2007-07-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1990-09-01 00:00:00
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pub_type: 杂志文章
doi:10.21873/anticanres.14762
更新日期:2021-01-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章,随机对照试验
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更新日期:2019-10-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章,评审
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更新日期:2019-07-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2009-11-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2004-03-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章,多中心研究
doi:
更新日期:1999-07-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2014-10-01 00:00:00
abstract::The antineoplastic drug 4'-iodo-4'-deoxydoxorubicin (IDX), a new halogenated anthracycline (1), was examined as a differentiation inducing agent on the human neuroblastoma cell lines TS12 and SK-N-MC. IDX induced morphological and biochemical differentiation and growth inhibition. The effect of a combined treatment of...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1991-09-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2000-11-01 00:00:00
abstract::Hyperthermia is effective for the treatment of cancer when applied concomitantly with chemotherapy and irradiation. However, it is difficult to heat deep portions of the body including the esophagus. Cancer of the esophagus still poses considerable treatment problems, with a poor 5-year survival rate after surgery, an...
journal_title:Anticancer research
pub_type: 临床试验,杂志文章,评审
doi:
更新日期:1992-05-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1997-11-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1998-07-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2006-01-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2008-05-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1995-09-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2014-09-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章,评审
doi:
更新日期:1990-03-01 00:00:00
abstract:BACKGROUND:Calpains (CAPN) are intracellular, non-lysosomal cytoplasmic cysteine endopeptidases and they are expressed ubiquitously. Their endogenous specific inhibitor is calpastatin. When calcium is present, calpastatin and calpain attach to each other, inhibiting the protease. The calpain system plays an important r...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2010-07-01 00:00:00
abstract:BACKGROUND/AIM:Few data are available on the utility of definitive radiation therapy (RT) for pediatric craniopharyngioma. This study sought to evaluate practice patterns and patient outcomes using the Surveillance Epidemiology and End Results database from 2004-2014. MATERIALS AND METHODS:Overall survival (OS) was co...
journal_title:Anticancer research
pub_type: 杂志文章
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更新日期:2019-02-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章,评审
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更新日期:2017-05-01 00:00:00
abstract::An immunohistochemical study of 155 squamous cell carcinomas of the oesophagus, squamous epithelium adjacent to the tumour (n = 80), dysplastic epithelium (n = 16) and controls (n = 23) indicates that Ki67 and p53 expression is frequently present in premalignant oesophageal lesions and their related squamous cell carc...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1994-01-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2002-11-01 00:00:00