Inhibitory potency of lithocholic acid analogs and other bile acids on glucuronosyltransferase activity in a colon cancer cell line

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DOIResolve DOI: http://doi.org/10.1016/0960-894X(96)00092-3
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TypeArticle
Journal titleBioorganic & Medicinal Chemistry Letters
Volume6
Issue6
Pages637642; # of pages: 6
AbstractThe effectiveness of analogs of lithocholic acid and other bile acids in inhibiting glucuronosyltransferase activity in a colon cancer cell line was measured in order to identify structural features critical for inhibition of the enzyme. Analogs of lithocholic acid with modifications of the side chain (2-7) were synthesized, in part, to study their inhibitory effects on glucuronosyltransferase activity. Bishomolithocholic acid (4) was synthesized from the iodo derivative (9) by a free radical Michael type reaction using tris(trimethylsilyl)silane as a free radical mediator. The effectiveness of analogs of lithocholic acid and other bile acids on glucuronosyltransferase activity in a colon cancer cell line was measured in order to identify structural features critical for the inhibition. Analogs of lithocholic acid (2-7) were synthesized with modifications of the side chain. Bishomolithocholic acid (4) was synthesized from the iodo derivative (9) by a free radical Michael type reaction-using tris(trimethylsilyl)silane as a free radical mediator.
Publication date
LanguageEnglish
AffiliationNational Research Council Canada; NRC Institute for Biological Sciences; NRC Steacie Institute for Molecular Sciences
Peer reviewedNo
NRC numberSCHNEIDER1996
NPARC number12338704
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Record identifierbc7177ba-b4fa-4a7e-b561-457c83bc8a42
Record created2009-09-10
Record modified2016-05-09
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