Degradation-promoters of cellular inhibitor of apoptosis protein 1 based on bestatin and actinonin

Shinichi Sato, Masashi Tetsuhashi, Keiko Sekine, Hiroyuki Miyachi, Mikihiko Naito, Yuichi Hashimoto, Hiroshi Aoyama

研究成果: Article査読

19 被引用数 (Scopus)

抄録

A series of hybrid compounds of bestatin (1) and actinonin (3), which promote degradation of cellular inhibitor of apoptosis protein 1 (cIAP1), were designed and synthesized. Structure-activity relationship studies indicated that absolute configuration, hydrophobicity at the α-position of the internal amide carbonyl group, and the presence of a small substituent at the α-position of the ester group are important factors for the expression of potent cIAP1 degradation-promoting activity. HAB-5A (30b) showed the most potent activity (IC50 = 0.53 μM) among the compounds prepared.

本文言語English
ページ(範囲)4685-4698
ページ数14
ジャーナルBioorganic and Medicinal Chemistry
16
8
DOI
出版ステータスPublished - 2008 4 15
外部発表はい

ASJC Scopus subject areas

  • 生化学
  • 分子医療
  • 分子生物学
  • 薬科学
  • 創薬
  • 臨床生化学
  • 有機化学

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