Steroids

Probing the active site of aromatase with 2-methyl-substituted androstenedione analogs

M Numazawa, Y Watari, K Yamada, N Umemura…

文献索引：Numazawa, Mitsuteru; Watari, Yoko; Yamada, Keiko; Umemura, Nao; Handa, Wakako Steroids, 2003 , vol. 68, # 6 p. 503 - 513

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被引用次数: 13

摘要

To gain insight into the spatial nature of the androstenedione (AD) binding (active) site of aromatase in relation to the catalytic function of the enzyme, we synthesized 2, 2-dimethylAD (4), 2β-and 2α-methylADs (5 and 6), 19-oxygenated derivatives of compounds 4 and 6, and 2-methyleneAD (17), and we then tested their inhibitory activity as well as their aromatase reaction (aromatization for 2-methyl and 2-methylene analogs or 19-oxygenation for 2, 2- ...