Diphenylmethane skeleton as a multi-template for nuclear receptor ligands: preparation of FXR and PPAR ligands

Masahiko Kainuma; Jun-ichi Kasuga; Shinnosuke Hosoda; Ken-ichi Wakabayashi; Aya Tanatani; Kazuo Nagasawa; Hiroyuki Miyachi; Makoto Makishima; Yuichi Hashimoto

doi:10.1016/j.bmcl.2006.03.075

Diphenylmethane skeleton as a multi-template for nuclear receptor ligands: preparation of FXR and PPAR ligands

Bioorg Med Chem Lett. 2006 Jun 15;16(12):3213-8. doi: 10.1016/j.bmcl.2006.03.075. Epub 2006 Apr 17.

Authors

Masahiko Kainuma¹, Jun-ichi Kasuga, Shinnosuke Hosoda, Ken-ichi Wakabayashi, Aya Tanatani, Kazuo Nagasawa, Hiroyuki Miyachi, Makoto Makishima, Yuichi Hashimoto

Affiliation

¹ Institute of Molecular and Cellular Biosciences, University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.

PMID: 16617018
DOI: 10.1016/j.bmcl.2006.03.075

Abstract

Novel, potent farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor alpha (PPARalpha) agonists were obtained by using a diphenylmethane skeleton as a substitute for a steroid skeleton.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Benzhydryl Compounds / chemical synthesis
Benzhydryl Compounds / chemistry*
Benzhydryl Compounds / metabolism*
DNA-Binding Proteins / agonists*
DNA-Binding Proteins / genetics
DNA-Binding Proteins / metabolism*
Humans
Ligands
Molecular Structure
PPAR alpha / agonists*
PPAR alpha / metabolism*
Receptors, Cytoplasmic and Nuclear
Transcription Factors / agonists*
Transcription Factors / genetics
Transcription Factors / metabolism*
Transcription, Genetic / genetics

Substances

Benzhydryl Compounds
DNA-Binding Proteins
Ligands
PPAR alpha
Receptors, Cytoplasmic and Nuclear
Transcription Factors
farnesoid X-activated receptor
diphenylmethane