Abstract：
BACKGROUND:5-Fluoro-2'-deoxyuridine (5-FdU), a drug against gastric cancer, was covalently linked via its nucleobase with the amino-bisphosphonate alendronate (Ale), resulting in a new antimetabolite-bisphosphonate conjugate (5-FdU-Ale), designed for bone-targeting. MATERIALS AND METHODS:The cytostatic effect of 5-FdU-Ale was evaluated in vitro compared to monomers and mixtures using CASY Technologies and the human gastric adenocarcinoma cell lines 23132/87 and MKN-45, in comparison to the intestinal CCL-241 and dermal fibroblast NHDF neonatal cell lines. RESULTS:The adenocarcinoma cell lines demonstrated a slightly higher sensitivity, with respect to the cell lines CCL-241 and NHDF, to incubation with 5-FdU-Ale. In comparison to 5-FdU, 5-FU and an equimolar mixture of Ale+5-FdU and Ale+5-FU, the cytostatic activity of the 5-FdU-Ale was markedly reduced. CONCLUSION:5-FdU-Ale was only partially or not at all metabolized to a mixture of cytostatic metabolites in vitro. Therefore an in vivo evaluation of the conjugates is indicated.
journal_name
Anticancer Resjournal_title
Anticancer researchauthors
Weinreich J,Schott TC,Königsrainer I,Küper M,Königsrainer A,Schott Hsubject
Has Abstractpub_date
2012-10-01 00:00:00pages
4299-305issue
10eissn
0250-7005issn
1791-7530pii
32/10/4299journal_volume
32pub_type
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journal_title：Anticancer research
pub_type： 临床试验,杂志文章
doi：
更新日期：1997-11-01 00:00:00
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journal_title：Anticancer research
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pub_type： 杂志文章
doi：
更新日期：2001-05-01 00:00:00
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更新日期：2010-04-01 00:00:00
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doi：
更新日期：2004-03-01 00:00:00
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doi：
更新日期：2010-01-01 00:00:00
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journal_title：Anticancer research
pub_type： 临床试验,杂志文章
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doi：
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doi：
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doi：
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