Probing the binding pocket of the active site of aromatase with 2-phenylaliphatic androsta-1, 4-diene-3, 17-dione steroids
M Takahashi, K Yamashita, M Numazawa
Index: Takahashi, Madoka; Yamashita, Kouwa; Numazawa, Mitsuteru Steroids, 2010 , vol. 75, # 4-5 p. 330 - 337
Full Text: HTML
Citation Number: 10
Abstract
A series of 2-phenylaliphatic-substituted androsta-1, 4-diene-3, 17-diones (6) as well as their androstenedione derivatives (5) were synthesized as aromatase inhibitors to gain insights of structure–activity relationships of varying the alkyl moiety (C1 to C4) of the 2- phenylaliphatic substituents as well as introducing a methyl-or trifluoromethyl function to p- position of a phenethyl moiety to the inhibitory activity. The inhibitors examined showed a ...
Related Articles:
Design and synthesis of phenethyl benzo [1, 4] oxazine-3-ones as potent inhibitors of PI3Kinaseγ
[Lanni Jr., Thomas B.; Greene, Keri L.; Kolz, Christine N.; Para, Kimberly S.; Visnick, Melean; Mobley, James L.; Dudley, David T.; Baginski, Theodore J.; Liimatta, Marya B. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 3 p. 756 - 760]
[Ornstein, Paul L.; Bleisch, Thomas J.; Arnold, M. Brian; Kennedy, Joseph H.; Wright, Rebecca A.; Johnson, Bryan G.; Tizzano, Joseph P.; Helton, David R.; Kallman, Mary Jeanne; Schoepp, Darryle D.; Herin, Marc Journal of Medicinal Chemistry, 1998 , vol. 41, # 3 p. 358 - 378]