501120-09-8Relevant articles and documents
Synthesis and biological evaluation of novel steroidal pyrazoles as substrates for bile acid transporters
Bhat, Laxminarayan,Jandeleit, Bernd,Dias, Tracy M.,Moors, Tristen L.,Gallop, Mark A.
, p. 85 - 87 (2007/10/03)
A series of novel C2-C3 annulated steroidal pyrazoles was synthesized as substrates for bile acid transporters. The pyrazoles were conjugated with drugs and drug surrogates. Their in vitro transport activities were evaluated in human ileal bile acid transporter (hIBAT) and human liver bile acid transporter (hLBAT) systems. The results of synthetic and transporter assay studies are described. A series of novel steroidal pyrazoles was synthesized as substrates for bile acid transporters to explore their potential as drug carriers. The selected pyrazole fused bile acids were further conjugated with drugs and drug surrogates. Their in vitro transport activities were evaluated in human ileal bile acid transporter (hIBAT) and human liver bile acid transporter (hLBAT) expressing Chinese hamster ovary (CHO)-cells and Xenopus laevis oocytes. The results of synthetic efforts and transporter assays studies are described herein.