EMAIL THIS PAGE TO A FRIEND

Journal of medicinal chemistry

Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators.


PMID 19856921

Abstract

Herein we describe the discovery of ACP-105 (1), a novel and potent nonsteroidal selective androgen receptor modulator (SARM) with partial agonist activity relative to the natural androgen testosterone. Compound 1 was developed from a series of compounds found in a HTS screen using the receptor selection and amplification technology (R-SAT). In vivo, 1 improved anabolic parameters in a 2-week chronic study in castrated male rats. In addition to compound 1, a number of potent antiandrogens were discovered from the same series of compounds whereof one compound, 13, had antagonist activity at the AR T877A mutant involved in prostate cancer.

Related Materials

Product #

Image

Description

Molecular Formula

Add to Cart

T5411
Testosterone solution, 1.0 mg/mL in 1,2-dimethoxyethane, drug standard