Synthesis and Pharmacological Evaluation of Novel Arylpiperazine Derivatives as Nonsteroidal Androgen Receptor Antagonists
The search for novel antiandrogens by high-throughput screening (HTS) of the Yamanouchi chemical library led to the discovery of the lead compound (5), which possesses an arylmorpholine moiety. Through the optimization of the lead compound (5), we have found a series of novel arylpiperazine derivati...
Saved in:
Published in | Chemical & Pharmaceutical Bulletin Vol. 52; no. 11; pp. 1330 - 1333 |
---|---|
Main Authors | , , , , , , |
Format | Journal Article |
Language | English Japanese |
Published |
TOKYO
The Pharmaceutical Society of Japan
01.11.2004
Pharmaceutical Society of Japan Pharmaceutical Soc Japan Japan Science and Technology Agency |
Subjects | |
Online Access | Get full text |
Cover
Loading…
Summary: | The search for novel antiandrogens by high-throughput screening (HTS) of the Yamanouchi chemical library led to the discovery of the lead compound (5), which possesses an arylmorpholine moiety. Through the optimization of the lead compound (5), we have found a series of novel arylpiperazine derivatives. Among them, 4-[4-cyano-(3-trifluoromethyl)phenyl]-N-(4-fluorophenyl)piperazine-1-carboxamide (22; YM-92088) exhibited a potent AR antagonistic activity with an IC50 value of 0.47 μM in the reporter assay, which is more potent than bicalutamide (4) which has an IC50 value of 0.89 μM. |
---|---|
Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0009-2363 1347-5223 |
DOI: | 10.1248/cpb.52.1330 |