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Development of a Benzopyran‐Containing Androgen Receptor Antagonist to Treat Antiandrogen‐Resistant Prostate Cancer
Author(s) -
Oh Sangmi,
Nam Hye Jin,
Park Jongmin,
Beak Sung Hee,
Park Seung Bum
Publication year - 2010
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200900509
Subject(s) - lncap , prostate cancer , antiandrogen , androgen receptor , antagonist , prostate , androgen , cancer research , pharmacology , medicine , cancer , hormone , receptor
Antagonizing cancer! 2 000 druglike small molecules were screened and a scaffold identified as a potentially novel androgen receptor antagonist framework. A focused library of 19 derivatives was then synthesized and evaluated in vitro against LNCaP prostate cancer cell line. A novel compound ( 6 f ) was identified as a promising lead compound for the further development of new therapeutic agents against hormone‐refractory prostate cancer.