INHIBITORY POTENCY OF LITHOCHOLIC ACID ANALOGS AND OTHER BILE-ACIDS ON GLUCURONOSYLTRANSFERASE ACTIVITY IN A COLON-CANCER CELL-LINE

Authors
SCHNEIDER H FIANDER H HARRISON KA WATSON M BURTON GW ARYA P
Citation
H. Schneider et al., INHIBITORY POTENCY OF LITHOCHOLIC ACID ANALOGS AND OTHER BILE-ACIDS ON GLUCURONOSYLTRANSFERASE ACTIVITY IN A COLON-CANCER CELL-LINE, Bioorganic & medicinal chemistry letters, 6(6), 1996, pp. 637-642
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
6
Year of publication
1996
Pages
637 - 642
Database
ISI
SICI code
0960-894X(1996)6:6<637:IPOLAA>2.0.ZU;2-A
Abstract
The 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 fo r inhibition of the enzyme. Analogs of lithocholic acid with modificat ions of the side chain (2-7) were synthesized, in part, to study their inhibitory effects on glucuronosyltransferase activity. Bishomolithoc holic acid (4) was synthesized from the iodo derivative (9) by a free radical Michael type reaction using tris(trimethylsilyl)silane as a fr ee radical mediator.