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  • Title: Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators.
    Author: Hamann LG, Manfredi MC, Sun C, Krystek SR, Huang Y, Bi Y, Augeri DJ, Wang T, Zou Y, Betebenner DA, Fura A, Seethala R, Golla R, Kuhns JE, Lupisella JA, Darienzo CJ, Custer LL, Price JL, Johnson JM, Biller SA, Zahler R, Ostrowski J.
    Journal: Bioorg Med Chem Lett; 2007 Apr 01; 17(7):1860-4. PubMed ID: 17292608.
    Abstract:
    Pharmacokinetic studies in cynomolgus monkeys with a novel prototype selective androgen receptor modulator revealed trace amounts of an aniline fragment released through hydrolytic metabolism. This aniline fragment was determined to be mutagenic in an Ames assay. Subsequent concurrent optimization for target activity and avoidance of mutagenicity led to the identification of a pharmacologically superior clinical candidate without mutagenic potential.
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