Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands

Xuqing Zhang; Xiaojie Li; George F Allan; Amy Musto; Scott G Lundeen; Zhihua Sui

doi:10.1016/j.bmcl.2006.03.047

Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands

Bioorg Med Chem Lett. 2006 Jun 15;16(12):3233-7. doi: 10.1016/j.bmcl.2006.03.047. Epub 2006 Apr 5.

Authors

Xuqing Zhang¹, Xiaojie Li, George F Allan, Amy Musto, Scott G Lundeen, Zhihua Sui

Affiliation

¹ Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, LLC, 1000 Route 202, Raritan, NJ 08869, USA. xzhang5@prdus.jnj.com

PMID: 16603353
DOI: 10.1016/j.bmcl.2006.03.047

Abstract

A novel series of tetracyclic indoles have been designed, synthesized and evaluated as androgen receptor (AR) ligands. Studies of structure-activity relationships (SARs) were investigated, which led to some compounds in this series as strong binders to androgen receptors.

MeSH terms

Androgen Receptor Antagonists
Animals
Cell Line
Cyclization
Indoles / chemical synthesis
Indoles / chemistry*
Indoles / pharmacology*
Ligands
Mice
Molecular Structure
Rats
Receptors, Androgen / metabolism*
Structure-Activity Relationship

Substances

Androgen Receptor Antagonists
Indoles
Ligands
Receptors, Androgen
indole