Matches in UGent Biblio for { <https://biblio.ugent.be/publication/3257351#aggregation> ?p ?o. }
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- aggregation classification "C3".
- aggregation creator B98975.
- aggregation creator person.
- aggregation creator person.
- aggregation creator person.
- aggregation creator person.
- aggregation date "2012".
- aggregation hasFormat 3257351.bibtex.
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- aggregation hasFormat 3257351.dc.
- aggregation hasFormat 3257351.didl.
- aggregation hasFormat 3257351.doc.
- aggregation hasFormat 3257351.json.
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- aggregation hasFormat 3257351.txt.
- aggregation hasFormat 3257351.xls.
- aggregation hasFormat 3257351.yaml.
- aggregation language "eng".
- aggregation subject "Chemistry".
- aggregation title "A convenient and versatile route to 2-alkyl-19-nor-analogs of calcitriol".
- aggregation abstract "Since decades, researchers have been intrigued by 1α,25-dihydroxy vitamin D3 (calcitriol) in various important cellular processes. Apart from its well-known role in calcium- and phosphate-regulation, this steroid metabolite presents also a remarkably broad spectrum of effects. Most notably, its unique property to both inhibit cell proliferation and promote cell differentiation that has drawn a lot of interest for this hormone as a possible small molecule-based, non-cytotoxic treatment for cancers. The responsible drug target, the vitamin D receptor (VDR), is found in over 30 different tissues in the human body, including various tumors, opening up a whole range of therapeutic areas. However, dosing test animals with the required supra-fysiological amounts of calcitriol causes acute hypercalcemia leading to bone deformation, hardening of soft organs and eventually mortality. Labour-intensive SAR studies on the complex vitamin D scaffold established that calcemic activities could be separated from the therapeutic activities by analoging. In fact, analogues are now used clinically: for example inecalcitol, first synthesized in our group, and which showed remarkably low calcemic effect in animal models. This possible future medicine has now reached phase IIb clinical trials in the treatment of prostate cancer. We have shown that two calcitriol modifications, where a methyl or ethyl group is introduced at the 2α-position, had some of the lowest in vivo (calcemic) toxicities in mice, while remaining very potent in in vitro assays on inhibition of human cancer cell growth. However, the initially developed synthetic routes were highly inefficient and only gave sub-milligram amounts of these analogues. Here, we will present a practical route for novel A-ring building blocks, starting from quinic acid allowing larger scale synthesis of these sort of analogues, as required for studies in animal models of various diseases. Such extensive in vivo tests on these promising 2-ethyl analogues are now in progress at the KULeuven.".
- aggregation authorList BK254377.
- aggregation isDescribedBy 3257351.
- aggregation similarTo LU-3257351.