Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands.
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.
Zhang
Xuqing
X
Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, LLC, 1000 Route 202, Raritan, NJ 08869, USA. xzhang5@prdus.jnj.com
Li
Xiaojie
X
Allan
George F
GF
Musto
Amy
A
Lundeen
Scott G
SG
Sui
Zhihua
Z
D059002:Androgen Receptor Antagonists; D000818:Animals; D002460:Cell Line; D003500:Cyclization; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008024:Ligands; D051379:Mice; D015394:Molecular Structure; D051381:Rats; D011944:Receptors, Androgen / Q000378:metabolism*; D013329:Structure-Activity Relationship
D059002:Androgen Receptor Antagonists; D007211:Indoles; D008024:Ligands; D011944:Receptors, Androgen; C030374:indole