title: Arylsulfonylamino-benzanilides as inhibitors of the apical sodium-dependent bile salt transporter (SLC10A2).
abstract: The apical sodium-dependent bile salt transporter (ASBT) plays a pivotal role in maintaining bile acid homeostasis. Inhibition of ASBT would reduce bile acid pool size and lower cholesterol levels. In this report, a series of novel arylsulfonylaminobenzanilides were designed and synthesized as potential inhibitors of ASBT. Most of them demonstrated great potency against ASBT's bile acid transport activity. In particular, compound 5g₂ inhibited ASBT activity with an IC₅₀ value of 0.11 μM. These compounds represent potential cholesterol-lowering drugs.
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
authors.forename: Hong-Tao
authors.initials: HT
authors.lastname: Liu
authors.forename: Hong-Wei
authors.initials: HW
authors.lastname: He
authors.forename: Xiao-Guang
authors.initials: XG
authors.lastname: Bai
authors.forename: Ju-Xian
authors.initials: JX
authors.lastname: Wang
authors.forename: Chang-Liang
authors.initials: CL
authors.lastname: Xu
authors.forename: Shi-Ying
authors.initials: SY
authors.lastname: Cai
authors.forename: Rong-Guang
authors.initials: RG
authors.lastname: Shao
authors.forename: Yu-Cheng
authors.initials: YC
authors.lastname: Wang
mesh_terms: D000813:Anilides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001190:Arylsulfonates / Q000737:chemistry*; D002460:Cell Line; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D029363:Organic Anion Transporters, Sodium-Dependent / Q000037:antagonists & inhibitors*; D027981:Symporters / Q000037:antagonists & inhibitors*
chemical_list: D000813:Anilides; D001190:Arylsulfonates; D029363:Organic Anion Transporters, Sodium-Dependent; D027981:Symporters; C071908:sodium-bile acid cotransporter; C034595:benzanilide