C 17, 20-Lyase inhibitors I. Structure-based de novo design and SAR study of C 17, 20-lyase inhibitors

N Matsunaga, T Kaku, F Itoh, T Tanaka, T Hara…

文献索引：Matsunaga, Nobuyuki; Kaku, Tomohiro; Itoh, Fumio; Tanaka, Toshimasa; Hara, Takahito; Miki, Hiroshi; Iwasaki, Masahiko; Aono, Tetsuya; Yamaoka, Masuo; Kusaka, Masami; Tasaka, Akihiro Bioorganic and medicinal chemistry, 2004 , vol. 12, # 9 p. 2251 - 2273

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被引用次数: 40

摘要

Novel nonsteroidal C17, 20-lyase inhibitors were synthesized using de novo design based on its substrate, 17α-hydroxypregnenolone, and several compounds exhibited potent C17, 20-lyase inhibition. However, in vivo activities were found to be short-lasting, and in order to improve the duration of action, a series of benzothiophene derivatives were evaluated. As a result, compounds 9h,(S)-9i, and 9k with nanomolar enzyme inhibition (IC50= 4–9nM) and ...