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2005
Pyrazine derivatives
R 0550
The Synthesis and Evaluation of [2.2.1]-Bicycloazahydantoins as Androgen
Antagonists. — The design and synthesis of the modified bicyclic hydanto16- 145 Receptor
ins (X) and (XI) is carried out, based on the biological activity of the parental ring-system and molecular modeling utilizing the crystal structure of dihydro-testosterone
bound to the wild-type androgen receptor. Endo-isomers (X) display increased binding
to the androgen receptor compared to the exo-isomers (XI). On the other hand, exo-isomers (XI) are slightly more potent in the functional activity assay but neither compares
well to the reference compound. Hydantoins (XII), synthesized from a compound having the same structure pattern as (X), show improved antagonistic activity against
the wild-type cell line compared to (XI). — (BALOG*, A.; et al.; Bioorg. Med.
Chem. Lett. 14 (2004) 24, 6107-6111; Dep. Oncol. Chem., Bristol-Myers Squibb
Pharm. Res. Inst., Princeton, NJ 08543, USA; Eng.) — H. Hoennerscheid
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